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  • Dose-Response Relationship, Drug  (89)
  • Structure-Activity Relationship  (85)
  • American Association for the Advancement of Science (AAAS)  (167)
  • Annual Reviews
  • Cambridge University Press
  • International Union of Crystallography (IUCr)
  • 1980-1984  (167)
  • 1970-1974
  • 1955-1959
  • 1930-1934
Collection
Keywords
Publisher
  • American Association for the Advancement of Science (AAAS)  (167)
  • Annual Reviews
  • Cambridge University Press
  • International Union of Crystallography (IUCr)
Years
Year
  • 1
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    Bioactive conformation of luteinizing hormone-releasing hormone: evidence from a conformationally constrained analog (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-11-07
    Description: An analog of luteinizing hormone-releasing hormone containing a gamma-lactam as a conformational constraint has been prepared with the use of a novel cyclization of a methionine sulfonium salt. The analog is more active as a luteinizing hormone-releasing hormone agonist that the parent hormone, and provides evidence for a bioactive conformation containing a beta-turn.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Freidinger, R M -- Veber, D F -- Perlow, D S -- Brooks, J R -- Saperstein, R -- New York, N.Y. -- Science. 1980 Nov 7;210(4470):656-8.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7001627" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Animals ; Biological Assay ; Cells, Cultured ; Female ; *Gonadotropin-Releasing Hormone/analogs & derivatives ; Hydrogen Bonding ; Lactams ; Protein Conformation ; Rats ; Structure-Activity Relationship
    Print ISSN: 0036-8075
    Electronic ISSN: 1095-9203
    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 2
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    Three-dimensional molecular modeling and drug design (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-06-27
    Description: A discussion of drug-receptor theory is used to show that the three-dimensional structure, or shape, of molecules is important for biological activity. The computer-assisted molecular modeling system at Merck is described, and it is shown that this system is useful for generating and storing molecular structures, determining preferred conformation, comparing molecular shapes, and computing molecular properties. Applications of the system to the study of anti-inflammatory drugs, somatostatin-like compounds, and dihydrofolate reductase inhibitors are summarized.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Gund, P -- Andose, J D -- Rhodes, J B -- Smith, G M -- New York, N.Y. -- Science. 1980 Jun 27;208(4451):1425-31.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6104357" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Arachidonic Acids ; Binding Sites ; Computers ; Cyclooxygenase Inhibitors ; Humans ; Indomethacin ; *Models, Molecular ; *Models, Structural ; *Molecular Conformation ; *Pharmaceutical Preparations ; Receptors, Drug/metabolism ; Somatostatin/analogs & derivatives ; Structure-Activity Relationship
    Print ISSN: 0036-8075
    Electronic ISSN: 1095-9203
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  • 3
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    Survival of mice receiving melanoma transplants is promoted by hydroquinone (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-04-25
    Description: In BALB/c female mice with melanoma transplants, the incidence of "takes" is decreased and survival is increased by hydroquinone, a melanocytolytic agent. The mechanism of drug action is suggested by via DNA. The significant and high degree of positive response to hydroquinone treatment in vivo is encouraging for the clinical management of melanoma with melanocytolytic agents.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Chavin, W -- Jelonek, E J Jr -- Reed, A H -- Binder, L R -- New York, N.Y. -- Science. 1980 Apr 25;208(4442):408-10.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7367868" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Disease Models, Animal ; Dose-Response Relationship, Drug ; Female ; Hydroquinones/metabolism/*therapeutic use ; Melanocytes/metabolism ; Melanoma/*drug therapy ; Mice ; Neoplasm Transplantation ; Neoplasms, Experimental/drug therapy
    Print ISSN: 0036-8075
    Electronic ISSN: 1095-9203
    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 4
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    Oral contraceptives, lanosterol, and platelet hyperactivity in rat (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-11-07
    Description: Lanosterol, a cholesterol precursor that increases considerably in the platelets of rats treated with oral contraceptives, was incubated with either platelet-rich plasma or washed platelet suspension. After 2 minutes there was a remarkable dose-related increase in platelet activity. This platelet hyperactivity was measured by clotting time and platelet aggregation could not be reproduced by cholesterol or ethinylestradiol.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Ciavatti, M -- Dumont, E -- Benoit, C -- Renaud, S -- New York, N.Y. -- Science. 1980 Nov 7;210(4470):642-4.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7433990" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Blood Coagulation/*drug effects ; Blood Platelets/*drug effects ; Contraceptives, Oral/*pharmacology ; Dose-Response Relationship, Drug ; Female ; Lanosterol/*pharmacology ; Platelet Aggregation/*drug effects ; Rats
    Print ISSN: 0036-8075
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    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 5
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    Vesicle targeting: timed release and specificity for leukocytes in mice by subcutaneous injection (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-01-18
    Description: When unilamellar vesicles were administered subcutaneously in mice, the half-time for the destruction of the vesicles varied from 12 to 600 hours, depending on their composition. The vesicles tested consisted of distearoyl phosphatidylcholine, cholesterol, and certain sugar and amino-sugar derivatives of cholesterol. Vesicle with amino-sugar derivatives showed the greatest longevity and became localized with high specificity in aggregates of polymorphonuclear leukocytes. A substantial delay between the time that the vesicles broke open and the time that labels contained in the vesicles were excreted suggests that the vesicles undergo endocytosis before destruction.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Mauk, M R -- Gamble, R C -- Baldeschwieler, J D -- New York, N.Y. -- Science. 1980 Jan 18;207(4428):309-11.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7350660" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cholesterol/analogs & derivatives ; Endocytosis ; Liposomes/*therapeutic use ; Lysosomes/metabolism ; Metabolic Clearance Rate ; Mice ; Neutrophils/*metabolism ; Phosphatidylcholines ; Structure-Activity Relationship
    Print ISSN: 0036-8075
    Electronic ISSN: 1095-9203
    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 6
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    Mebendazole therapy of parenteral trichinellosis (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-03-14
    Description: Mebendazole was highly effective against the helminth parasite Trichinella spiralis in mice subjected to a 3-day course of treatment during the invasive and encystment phases of experimental trichinellosis. When treatment began either 2 or 4 weeks after the mice were inoculated with parasites, the number of larvae developing in the host musculature was greatly reduced by twice-daily oral administration of 3.125, 6.25, or 12.5 milligrams of mebendazole per kilogram of body weight.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉McCracken, R O -- Taylor, D D -- New York, N.Y. -- Science. 1980 Mar 14;207(4436):1220-2.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7355285" target="_blank"〉PubMed〈/a〉
    Keywords: Administration, Oral ; Animals ; Benzimidazoles/*therapeutic use ; Disease Models, Animal ; Dose-Response Relationship, Drug ; Larva ; Male ; Mebendazole/administration & dosage/*therapeutic use ; Mice ; Muscles/parasitology ; Trichinella/drug effects ; Trichinellosis/*drug therapy
    Print ISSN: 0036-8075
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  • 7
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    Regression of tumors in guinea pigs after treatment with synthetic muramyl dipeptides and trehalose dimycolate (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-04-25
    Description: A high incidence of tumor regression was observed in guinea pigs bearing transplantable, line-10 hepatocellular carcinomas when synthetic muramyl dipeptides combined with trehalose dimycolate in oil-in-water emulsions were injected directly into the tumors. These compounds are promising candidates to replace viable bacillus Calmette-Guerin in cancer immunotherapy in humans and animals.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉McLaughlin, C A -- Schwartzman, S M -- Horner, B L -- Jones, G H -- Moffatt, J G -- Nestor, J J Jr -- Tegg, D -- New York, N.Y. -- Science. 1980 Apr 25;208(4442):415-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7189295" target="_blank"〉PubMed〈/a〉
    Keywords: Acetylmuramyl-Alanyl-Isoglutamine/administration & dosage/*therapeutic use ; Animals ; Cord Factors/administration & dosage/*therapeutic use ; Drug Combinations ; Emulsions ; Glycolipids/*therapeutic use ; Glycopeptides/*therapeutic use ; Immunotherapy ; Liver Neoplasms, Experimental/*therapy ; Lymphatic Metastasis ; Structure-Activity Relationship
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  • 8
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    Substance P: does it produce analgesia or hyperalgesia? (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-04-18
    Description: In the hot plate test, substance P given intravenously at doses of 5 x 10-5 and 5 x 10-4 gram per kilogram caused analgesia, while lower doses caused hyperalgesia. The influence of substance P on nociception depended on the individual mouse's sensitivity to pain (control response latency). Analgesia was produced by substance P administered to mice with high sensitivity to thermic stimulation, whereas hyperalgesia occurred in mice whose control latencies were longer than normal. This result is interpreted as an indication that substance P is capable of normalizing responsiveness to pain and could be classified as a regulatory peptide.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Oehme, P -- Hilse, H -- Morgenstern, E -- Gores, E -- New York, N.Y. -- Science. 1980 Apr 18;208(4441):305-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6154313" target="_blank"〉PubMed〈/a〉
    Keywords: Acetates ; Animals ; Dose-Response Relationship, Drug ; Hot Temperature ; Hyperalgesia/*chemically induced ; Hyperesthesia/*chemically induced ; Mice ; Nociceptors/drug effects ; Pain/*physiopathology ; Perception/*drug effects ; Receptors, Drug/physiology ; Substance P/*pharmacology
    Print ISSN: 0036-8075
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  • 9
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    alpha-Lactalbumin-casein induction in virgin mouse mammary explants: dose-dependent differential action of cortisol (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-03-21
    Description: The interplay of insulin, cortisol, and prolactin induces synthesis of casein and alpha-lactalbumin in cultured mammary explants from mature virgin mice. A striking difference has been found between the optimal concentrations of cortisol required for maximal induction of the two milk proteins in vitro: 3 x 10(-8) molar for alpha-lactalbumin and 3 x 10(-6) molar for casein. Moreover, 10(-7) to 10(-5) molar cortisol caused progressive inhibition of alpha-lactalbumin accumulation. Such differential actions of cortisol may partly account for the asynchronous synthesis of the two proteins during pregnancy.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Ono, M -- Oka, T -- New York, N.Y. -- Science. 1980 Mar 21;207(4437):1367-9.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6986657" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Caseins/*biosynthesis ; Dose-Response Relationship, Drug ; Drug Interactions ; Female ; Hydrocortisone/*pharmacology ; Insulin/pharmacology ; Lactalbumin/*biosynthesis ; Mammary Glands, Animal/drug effects/*metabolism ; Mice ; Organ Culture Techniques ; Pregnancy ; Prolactin/pharmacology
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  • 10
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    Kindling induces long-lasting alterations in response of hippocampal neurons to elevated potassium levels in vitro (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-06-13
    Description: The cellular basis of kindling was studied electrophysiologically with slices of guinea pig hippocampus. Normally, epileptiform activity can be induced in the slices only by combined exposure to elevated potassium levels and a chemical convulsant such as penicillin. In hippocampal slices from pentylenetetrazole-kindled animals, however, elevated potassium alone can induce seizures. These data suggest that kindling elicits long-term changes in neuronal excitability that may involve ionic mechanisms.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Oliver, A P -- Hoffer, B J -- Wyatt, R J -- New York, N.Y. -- Science. 1980 Jun 13;208(4449):1264-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7375936" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Dose-Response Relationship, Drug ; Epilepsy/chemically induced/*physiopathology ; Guinea Pigs ; Hippocampus/drug effects/*physiology ; In Vitro Techniques ; Male ; Neurons/drug effects/physiology ; Pentylenetetrazole/administration & dosage/pharmacology ; Potassium/*pharmacology
    Print ISSN: 0036-8075
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  • 11
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    Food dyes impair performance of hyperactive children on a laboratory learning test (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-03-28
    Description: Forty children were given a diet free of artificial food dyes and other additives for 5 days. Twenty of the children had been classified as hyperactive by scores on the Conners Rating Scale and were reported to have favorable responses to stimulant medication. A diagnosis of hyperactivity had been rejected in the other 20 children. Oral challenges with large doses (100 or 150 milligrams) of a blend of FD & C approved food dyes or placebo were administered on days 4 and 5 of the experiment. The performance of the hyperactive children on paired-associate learning tests on the day they received the dye blend was impaired relative to their performance after they received the placebo, but the performance of the nonhyperactive group was not affected by the challenge with the food dye blend.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Swanson, J M -- Kinsbourne, M -- New York, N.Y. -- Science. 1980 Mar 28;207(4438):1485-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7361102" target="_blank"〉PubMed〈/a〉
    Keywords: Child ; Dose-Response Relationship, Drug ; Female ; Food Coloring Agents/*pharmacology ; Humans ; Hyperkinesis/*physiopathology ; Learning/*drug effects ; Male ; Time Factors
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  • 12
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    Stereospecific nicotine receptors on rat brain membranes (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-11-07
    Description: A stereospecific binding site for nicotine has been detected on rat brain membranes. Competition studies with cholinergic agonists suggest that this site is a nicotinic cholinergic receptor.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Romano, C -- Goldstein, A -- DA-1938/DA/NIDA NIH HHS/ -- DA-7063/DA/NIDA NIH HHS/ -- New York, N.Y. -- Science. 1980 Nov 7;210(4470):647-50.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7433991" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Binding, Competitive ; Brain/*metabolism ; Ligands ; Male ; Nicotine/metabolism ; Rats ; Receptors, Cholinergic/*metabolism ; Receptors, Nicotinic/*metabolism ; Stereoisomerism ; Structure-Activity Relationship ; Synaptic Membranes/metabolism
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  • 13
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    Genotoxicity of the antihypertensive drugs hydralazine and dihydralazine (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-10-17
    Description: The genotoxicity of the antihypertensive agents hydralazine and dihydralazine was tested in mammalian cells and bacteria. Both drugs elicited DNA repair in rat hepatocyte primary cultures. In the Ames test, both with and without an S-9 fraction, hydralazine was mutagenic in strains TA100 and TA1537, whereas dihydralazine was weakly mutagenic in strain TA1537. These findings support the observation that hydralazine is carcinogenic in mice. The carcinogenicity of many chemicals results from interaction with DNA. Since these studies demonstrate that hydralazine and dihydralazine damage DNA in mammalian cells, these drugs should be viewed as potential human carcinogens.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Williams, G M -- Mazue, G -- McQueen, C A -- Shimada, T -- N 01-CP-55705/CP/NCI NIH HHS/ -- New York, N.Y. -- Science. 1980 Oct 17;210(4467):329-30.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7423193" target="_blank"〉PubMed〈/a〉
    Keywords: Acetylation ; Animals ; Biotransformation ; *Carcinogens ; Cells, Cultured ; DNA Repair/*drug effects ; Dihydralazine/*toxicity ; Dose-Response Relationship, Drug ; Drug Evaluation, Preclinical ; Hydralazine/*analogs & derivatives/*toxicity ; Liver/metabolism ; *Mutagens ; Rats ; Salmonella typhi/drug effects
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  • 14
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    Multiple daily amphetamine administration: behavioral and neurochemical alterations (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-02-15
    Description: In rats, multiple daily amphetamine injections (2.5 milligrams per kilogram of body weight, injected subcutaneously every 4 hours for 5 days) resulted in a progressive augmentation in response, characterized by a more rapid onset and an increased magnitude of stereotypy. By contrast, offset times of both the stereotypy and the poststereotypy hyperactivity periods were markedly shortened. When the animals were retested with the same dose of amphetamine 8 days after the long-term treatment was discontinued, the time of offset of the stereotypy and hyperactivity phases had recovered to values found with short-term amphetamine treatment, whereas the more rapid onset of stereotypy persisted. Brain monoamine and amphetamine concentrations and tyrosine hydroxylase activity were determined in comparably treated rats at times corresponding to the behavioral observations. The behavioral data indicate that enhanced responsiveness to amphetamine following its repeated administration may contribute to the development of amphetamine psychosis.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Segal, D S -- Weinberger, S B -- Cahill, J -- McCunney, S J -- New York, N.Y. -- Science. 1980 Feb 15;207(4433):905-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7188815" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Behavior/*drug effects ; Behavior, Animal/*drug effects ; Brain/metabolism ; Brain Chemistry/drug effects ; Dextroamphetamine/administration & dosage/*pharmacology ; Dopamine/metabolism ; Dose-Response Relationship, Drug ; Humans ; Male ; Motor Activity/drug effects ; Norepinephrine/metabolism ; Rats ; Serotonin/metabolism ; Stereotyped Behavior/*drug effects ; Time Factors
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  • 15
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    GABA analogues activate channels of different duration on cultured mouse spinal neurons (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-04-17
    Description: Voltage-clamp recordings from mouse spinal neurons grown in culture were used to study the membrane current fluctuations induced by 12 substances structurally similar to gamma-aminobutyric acid (GABA). Fluctuation analysis provided estimates of the electrical properties of the elementary events underlying these responses. Estimates of the mean conductance of channels activated by all of the substances except glycine did not differ significantly from that estimated for GABA, whereas mean durations of agonist-activated channels all differed significantly from that found for GABA. The results indicate that all of the substances tested except glycine activate channels of similar conductance but of different durations.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Barker, J L -- Mathers, D A -- New York, N.Y. -- Science. 1981 Apr 17;212(4492):358-61.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6259733" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cell Membrane/drug effects ; Ion Channels/*drug effects ; Membrane Potentials/drug effects ; Mice ; Neurons/drug effects ; Receptors, Cell Surface/metabolism ; Receptors, GABA-A ; Spinal Nerves/*drug effects ; Structure-Activity Relationship ; Time Factors ; gamma-Aminobutyric Acid/*analogs & derivatives/pharmacology
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  • 16
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    Multiple opiate receptors: alcohol selectively inhibits binding to delta receptors (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-10-23
    Description: The addition of ethanol or other aliphatic alcohols to rat brain membranes strongly inhibits binding of enkephalins at concentrations at which little inhibition of opiate alkaloids is seen. Inhibition is reversible, and potency increases with chain length of the alcohol. The results suggest that delta receptors are considerably more sensitive to alcohols than mu receptors. This is the first demonstration of selective inhibition of one of the postulated classes of opiate receptors by a reagent that is not a ligand for the receptor.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Hiller, J M -- Angel, L M -- Simon, E J -- DA-00017/DA/NIDA NIH HHS/ -- New York, N.Y. -- Science. 1981 Oct 23;214(4519):468-9.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6270788" target="_blank"〉PubMed〈/a〉
    Keywords: Alcohols/*pharmacology ; Animals ; Brain/metabolism ; Cells, Cultured ; In Vitro Techniques ; Neuroblastoma/metabolism ; Rats ; Receptors, Opioid/classification/*drug effects/metabolism ; Structure-Activity Relationship
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  • 17
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    Insulin as a potent, specific growth factor in a rat hepatoma cell line (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-02-27
    Description: A line or rat hepatoma cells in culture which, in response to serum starvation, become arrested in the early G1 phase of growth, can be stimulated by insulin alone to enter the cell cycle and traverse S phase. A half-maximum response is observed at 30 to 70 picomolar concentrations and the maximum response is essentially identical to that found with optimum serum concentrations.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Koontz, J W -- Iwahashi, M -- AM 24047/AM/NIADDK NIH HHS/ -- New York, N.Y. -- Science. 1981 Feb 27;211(4485):947-9.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7008195" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cell Cycle/drug effects ; Cell Division/drug effects ; Cell Line ; *Growth Substances ; Insulin/*pharmacology ; Liver Neoplasms, Experimental/*pathology ; Mitosis/drug effects ; Proinsulin/pharmacology ; Rats ; Structure-Activity Relationship
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  • 18
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    Rational approaches to chemotherapy: antisickling agents (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-08-14
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Klotz, I M -- Haney, D N -- King, L C -- New York, N.Y. -- Science. 1981 Aug 14;213(4509):724-31.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7256275" target="_blank"〉PubMed〈/a〉
    Keywords: Anemia, Sickle Cell/*drug therapy ; Aspirin/analogs & derivatives/therapeutic use ; Chemical Phenomena ; Chemistry ; *Hemoglobin, Sickle ; Humans ; Protein Binding/drug effects ; Protein Conformation ; Salicylates/*therapeutic use ; Solubility ; Structure-Activity Relationship
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  • 19
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    Asbestos surface charge heterogeneity and biological effects (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-09-25
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Light, W G -- New York, N.Y. -- Science. 1981 Sep 25;213(4515):1534.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7280676" target="_blank"〉PubMed〈/a〉
    Keywords: *Asbestos ; Humans ; Occupational Diseases/chemically induced ; Structure-Activity Relationship
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    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 20
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    Growth inhibition by adenosine 3',5-monophosphate derivatives does not require 3',5' phosphodiester linkage (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-09-04
    Description: Analogs of adenosine 3',5'-monophosphate (cyclic AMP) inhibit the growth of cultured cell lines. The effects of 8-bromo- and N6-butyryl-substituted analogs of cyclic and noncyclic AMP on six cell lines were examined and were equally inhibitory. Variant cell lines with altered cyclic AMP-dependent protein kinase were more resistant to both cyclic and noncyclic nucleotides. We conclude that growth inhibition by analogs of cyclic AMP (i) does not require a 3',5' phosphodiester bond and (ii) may be mediated by a pathway involving endogenous cyclic AMP.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Martin, T F -- Kowalchyk, J A -- AM 25861/AM/NIADDK NIH HHS/ -- New York, N.Y. -- Science. 1981 Sep 4;213(4512):1120-2.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6267695" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cell Division/*drug effects ; Cell Line ; Cricetinae ; Cyclic AMP/*pharmacology ; DNA/biosynthesis ; Growth Inhibitors/*pharmacology ; Mice ; Phosphodiesterase Inhibitors/pharmacology ; Structure-Activity Relationship
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  • 21
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    A new wave of antibiotics builds (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-12-11
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Maugh, T H -- New York, N.Y. -- Science. 1981 Dec 11;214(4526):1225-8.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7302591" target="_blank"〉PubMed〈/a〉
    Keywords: *Cephalosporins/therapeutic use ; Humans ; Research ; Structure-Activity Relationship ; United States
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  • 22
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    Thymosin stimulates secretion of luteinizing hormone-releasing factor (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-11-06
    Description: Partially purified thymosin fraction 5 and one of its synthetic peptide components, thymosin beta 4, but not thymosin alpha 1, stimulated secretion of luteinizing hormone--releasing factor from superfused medial basal hypothalami from random cycling female rats. In addition, luteinizing hormone was released from pituitary glands superfused in sequence with hypothalami. No release of luteinizing hormone in response to thymosin was observed from pituitaries superfused alone. These data provide the first evidence of a direct effect of the endocrine thymus on the hypothalamus and suggest a potentially important role for thymic peptides in reproductive function.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Rebar, R W -- Miyake, A -- Low, T L -- Goldstein, A L -- AG-01531/AG/NIA NIH HHS/ -- HD-12303/HD/NICHD NIH HHS/ -- HD-14362/HD/NICHD NIH HHS/ -- etc. -- New York, N.Y. -- Science. 1981 Nov 6;214(4521):669-71.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7027442" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Gonadotropin-Releasing Hormone/*secretion ; Hormones/pharmacology ; Hypothalamo-Hypophyseal System/drug effects ; Hypothalamus/*drug effects ; Peptide Fragments/pharmacology ; Rats ; Structure-Activity Relationship ; Thymosin/*pharmacology ; Thymus Hormones/*pharmacology
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    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 23
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    Didemnins: antiviral and antitumor depsipeptides from a caribbean tunicate (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-05-22
    Description: Extracts of samples of a Caribbean tunicate (ascidian, sea squirt) of the family Didemnidae inhibit in vitro at low concentrations the growth of DNA and RNA viruses as well as L1210 leukemic cells. The active compounds isolated from the tunicate, didemnins A, B, and C, are depsipeptides, and didemnin B (a derivative of didemnin A) is the component active at the lowest concentration in inhibiting viral replication in vitro and P388 leukemia in vivo.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Rinehart, K L Jr -- Gloer, J B -- Hughes, R G Jr -- Renis, H E -- McGovren, J P -- Swynenberg, E B -- Stringfellow, D A -- Kuentzel, S L -- Li, L H -- AI 04769/AI/NIAID NIH HHS/ -- GM 27029/GM/NIGMS NIH HHS/ -- New York, N.Y. -- Science. 1981 May 22;212(4497):933-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7233187" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Antibiotics, Antineoplastic/*isolation & purification ; Antiviral Agents/*isolation & purification ; *Depsipeptides ; Leukemia, Experimental/*drug therapy ; Peptides, Cyclic/*isolation & purification/therapeutic use ; Structure-Activity Relationship ; Urochordata/*analysis
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  • 24
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    2,4,5-trichlorophenoxyacetic acid causes behavioral effects in chickens at environmentally relevant doses (1981)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1981-02-06
    Description: Administration of the herbicide 2,4,5-trichlorophenoxyacetic acid to incubating chicken eggs alters behavior after hatching. Single doses, with no morphological effects, retard learning (lowest dose, 7 milligrams per kilogram of body weight) and increase general activity (27 milligrams per kilogram) and jumping (13 milligrams per kilogram). Day 15 of incubation is the most susceptible stage of development.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Sanderson, C A -- Rogers, L J -- New York, N.Y. -- Science. 1981 Feb 6;211(4482):593-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7455699" target="_blank"〉PubMed〈/a〉
    Keywords: 2,4,5-Trichlorophenoxyacetic Acid/*pharmacology/toxicity ; Age Factors ; Animals ; Behavior, Animal/*drug effects ; Chick Embryo/drug effects ; Chickens ; Discrimination Learning/drug effects ; Dose-Response Relationship, Drug ; Motor Activity/drug effects
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  • 25
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    Bee venom enhances guanylate cyclase activity (1981)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1981-07-17
    Description: Bee venom and phospholipase A2 extracted from bee venom enhanced guanylate cyclase (E.C. 4.6.1.2) activity two- to threefold in rat liver, lung, heart, kidney, ileum, and cerebellum. Dose-response relationships revealed that bee venom at concentrations as low as 1 microgram per milliliter and phospholipase A2 at 1 microunit per milliliter caused a maximal enhancement of guanylate cyclase.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Vesely, D L -- New York, N.Y. -- Science. 1981 Jul 17;213(4505):359-60.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6113689" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Bee Venoms/*pharmacology ; Dose-Response Relationship, Drug ; Enzyme Activation ; Guanylate Cyclase/*metabolism ; Kinetics ; Organ Specificity ; Phospholipases/*pharmacology ; Phospholipases A/*pharmacology ; Phospholipases A2 ; Rats
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  • 26
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    Chemical impurity produces extra compound eyes and heads in crickets (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-04-03
    Description: A chemical impurity isolated from commercially purchased acridine causes cricket embryos to develop extra compound eyes, branched antennae, extra antennae, and extra heads. Purified acridine does not produce similar duplications of cricket heads or head structures nor do the substituted acridines proflavine, acriflavine, or acridine orange. A dose-response relation exists such that the number and severity of abnormalities increase with increasing concentration of the teratogen.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Walton, B T -- New York, N.Y. -- Science. 1981 Apr 3;212(4490):51-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6782672" target="_blank"〉PubMed〈/a〉
    Keywords: Abnormalities, Multiple/chemically induced ; Acridines/*isolation & purification/pharmacology ; Animals ; Dose-Response Relationship, Drug ; Drug Contamination ; Embryo, Nonmammalian/drug effects ; Eye Abnormalities ; Head/abnormalities ; Orthoptera/*drug effects ; *Teratogens
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  • 27
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    Ethanol tolerance in the rat is learned (1981)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1981-07-31
    Description: Rats were trained to walk on a treadmill to avoid foot shock. The animals developed tolerance for ethanol if given subsequent practice while ethanol intoxicated. Rats given equivalent doses of ethanol after practice did not develop tolerance, nor did saline-treated controls. These results challenge the hypothesis that mere repeated doses of ethanol are sufficient to induce tolerance. It seems that tolerance does not develop unless the response used to measure tolerance is performed while the subject is intoxicated.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Wenger, J R -- Tiffany, T M -- Bombardier, C -- Nicholls, K -- Woods, S C -- 03504/PHS HHS/ -- AA 04658/AA/NIAAA NIH HHS/ -- New York, N.Y. -- Science. 1981 Jul 31;213(4507):575-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7244656" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Avoidance Learning/*drug effects ; Dose-Response Relationship, Drug ; Drug Tolerance ; Ethanol/blood/*pharmacology ; Rats
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  • 28
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    Micromolar affinity benzodiazepine receptors: identification and characterization in central nervous system (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-06-11
    Description: Receptors that selectively bind micromolar concentrations of benzodiazepines are present in rat brain membrane. These micromolar receptors exhibit saturable, stereospecific binding, and the potency of benzodiazepine binding to these receptors is correlated with the ability of the benzodiazepines to inhibit maximum electric shock-induced convulsions. Benzodiazepine receptors with nanomolar affinity differ from the micromolar receptors in their binding, kinetic, and pharmacologic characteristics. The micromolar receptors also bind phenytoin, a non-benzodiazepine anticonvulsant. These results provide evidence for a distinct class of clinically relevant benzodiazepine receptors that may regulate neuronal excitability and anticonvulsant activity.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Bowling, A C -- DeLorenzo, R J -- NS 1352/NS/NINDS NIH HHS/ -- New York, N.Y. -- Science. 1982 Jun 11;216(4551):1247-50.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6281893" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Benzodiazepines/*metabolism/pharmacology ; Benzodiazepinones/metabolism ; Brain/*metabolism ; Calmodulin/antagonists & inhibitors ; Diazepam/metabolism ; Kinetics ; Ligands ; Protein Kinase Inhibitors ; Rats ; Receptors, Drug/*metabolism ; Receptors, GABA-A ; Structure-Activity Relationship
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  • 29
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    Artificial enzymes (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-11-05
    Description: Simple chemical catalysts have been designed to achieve some desirable features of enzymes. These novel catalysts are not proteins, but they may incorporate the typical enzyme catalytic groups and they achieve selectivity in their reactions by use of geometric control, as do enzymes. Catalysts that carry out geometrically controlled chlorinations of aromatic rings and steroids have been constructed. Other catalysts achieve the selective synthesis of amino acids, and still others imitate ribonuclease in detailed mechanism and hydrolyze RNA. Optimization of geometries has led to a rate acceleration of over 10(8) in one instance.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Breslow, R -- New York, N.Y. -- Science. 1982 Nov 5;218(4572):532-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7123255" target="_blank"〉PubMed〈/a〉
    Keywords: Catalysis ; Cyclodextrins ; *Enzymes ; Kinetics ; Models, Chemical ; Ribonucleases ; Structure-Activity Relationship ; Substrate Specificity ; Transaminases
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    Stereoisomers of N-allylnormetazocine: phencyclidine-like behavioral effects in squirrel monkeys and rats (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-01-08
    Description: (+/-)-N-Allylnormetazocine is a benzomorphan opioid with psychotomimetic effects. The pure stereoisomers of this compound, as well as the racemic mixture, were compared to phencyclidine for their behavioral effects on squirrel monkeys and rats trained to discriminate phencyclidine from saline. Dose-response determinations were made for responses to phencyclidine, to a racemic mixture of N-allylnormetazocine, and to the pure levo and dextro isomers of N-allylnormetazocine. In both rats and monkeys, the dextro isomer and the racemic mixture produced dose-dependent responses appropriate for phencyclidine; the levo isomer did not produce the responses appropriate for phencyclidine at any of the doses tested. In both species, the levo isomer was more potent than the dextro isomer in decreasing the rate of responding. Thus racemic N-allylnormetazocine is a mixture of compounds that produce different behavioral effects.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Brady, K T -- Balster, R L -- May, E L -- DA-00490/DA/NIDA NIH HHS/ -- DA-01442/DA/NIDA NIH HHS/ -- New York, N.Y. -- Science. 1982 Jan 8;215(4529):178-80.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6274022" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Behavior, Animal/*drug effects ; Male ; Naloxone/pharmacology ; Phenazocine/*analogs & derivatives/pharmacology ; Phencyclidine/pharmacology ; Rats ; Rats, Inbred Strains ; Receptors, Opioid/drug effects ; Saimiri ; Stereoisomerism ; Structure-Activity Relationship
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  • 31
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    Calcium ionophore polarizes ooplasmic segregation in ascidian eggs (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-04-30
    Description: Calcium ionophore A23187 promotes ooplasmic segregation and orange crescent formation in eggs of the ascidian Boltenia villosa. When eggs were exposed to a gradient A23187 the orange crescent was induced to form in the region corresponding to the highest concentration of ionophore. This result is consistent with the hypothesis that a local increase in intracellular calcium polarizes cytoplasmic localization in the ascidian embryo.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Jeffery, W R -- 232-HDO-7098/HD/NICHD NIH HHS/ -- HD-13970/HD/NICHD NIH HHS/ -- New York, N.Y. -- Science. 1982 Apr 30;216(4545):545-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6803360" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Anti-Bacterial Agents/*pharmacology ; Calcimycin/*pharmacology ; Calcium/*physiology ; Cell Compartmentation/drug effects ; Cytoplasm/ultrastructure ; Dose-Response Relationship, Drug ; Female ; Ovum/*drug effects/ultrastructure ; Urochordata
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  • 32
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    Naloxone antagonism of the thermoregulatory effects of phencyclidine (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-09-24
    Description: Phencyclidine elicits hyperthermia at low doses and hypothermia at high doses in rats. Naloxone antagonizes both effects. Phencyclidine's effects on thermo-regulation are probably mediated by an interaction with a mu opiate receptor.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Glick, S D -- Guido, R A -- DA 02534/DA/NIDA NIH HHS/ -- DA 70082/DA/NIDA NIH HHS/ -- New York, N.Y. -- Science. 1982 Sep 24;217(4566):1272-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6287581" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Body Temperature Regulation/*drug effects ; Dose-Response Relationship, Drug ; Female ; Naloxone/pharmacology ; Phencyclidine/antagonists & inhibitors/*pharmacology ; Rats ; Receptors, Opioid/*drug effects
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  • 33
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    Alpha-substituted gamma-butyrolactones: new class of anticonvulsant drugs (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-09-10
    Description: Alkyl-Substituted gamma-butyrolactones were synthesized and tested for their convulsant and anticonvulsant actions in mice and guinea pigs. The alpha-substituted compounds, alpha, alpha-dimethyl-, and alpha-ethyl-alpha-methyl-gamma-butyrolactone were anticonvulsant compounds with a spectrum of activity similar to that of ethosuximide. In contrast, beta-substituted compounds were convulsant agents similar to picrotoxinin. The alpha-substituted-gama-butyrolactones represent a new class of anticonvulsant drug with experimental and clinical potential.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Klunk, W E -- McKeon, A -- Covey, D F -- Ferrendelli, J A -- GM-07200/GM/NIGMS NIH HHS/ -- GM-24483/GM/NIGMS NIH HHS/ -- NS-14834/NS/NINDS NIH HHS/ -- etc. -- New York, N.Y. -- Science. 1982 Sep 10;217(4564):1040-2.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6810462" target="_blank"〉PubMed〈/a〉
    Keywords: *4-Butyrolactone/analogs & derivatives/*therapeutic use/toxicity ; Animals ; *Anticonvulsants ; Chemical Phenomena ; Chemistry ; Convulsants ; Drug Evaluation, Preclinical ; Electroencephalography ; Epilepsy, Absence/drug therapy ; Ethosuximide/pharmacology ; *Furans/*therapeutic use ; Guinea Pigs ; Mice ; Structure-Activity Relationship ; Trimethadione/pharmacology
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  • 34
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    Purinergic regulation of food intake (1982)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1982-07-02
    Description: Inosine peripherally administered to rats markedly suppressed spontaneous food intake and food intake induced by diazepam, muscimol, insulin, and food deprivation. The purines 2-deoxyguanosine and 2-deoxyinosine also suppressed food deprivation-induced feeding, whereas 7-methylinosine, which does not bind to the benzodiazepine binding site in vitro, had no effect on food intake when compared with controls. These results suggest that purines may represent endogenous substances that regulate food intake through interactions with the benzodiazepine receptor.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Levine, A S -- Morley, J E -- New York, N.Y. -- Science. 1982 Jul 2;217(4554):77-9.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7046046" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Appetite/*drug effects ; Deoxyguanosine/pharmacology ; Diazepam/pharmacology ; Eating/*drug effects ; Food Deprivation ; Inosine/analogs & derivatives/pharmacology ; Insulin/pharmacology ; Male ; Muscimol/pharmacology ; Purines/*pharmacology ; Rats ; Rats, Inbred Strains ; Structure-Activity Relationship
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    Spectral character of sunlight modulates photosynthesis of previtamin D3 and its photoisomers in human skin (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-05-28
    Description: The photosynthesis of previtamin D3 from 7-dehydrocholesterol in human skin was determined after exposure to narrow-band radiation or simulated solar radiation. The optimum wavelengths for the production of previtamin D3 were determined to be between 295 and 300 nanometers. When human skin was exposed to 295-nanometer radiation, up to 65 percent of the original 7-dehydrocholesterol content was converted to previtamin D3. In comparison, when adjacent skin was exposed to simulated solar radiation, the maximum formation of previtamin D3 was about 20 percent. Major differences in the formation of lumisterol3, and tachysterol3 from previtamin D3 were also observed. It is concluded that the spectral character of natural sunlight has a profound effect on the photochemistry of 7-dehydrocholesterol in human skin.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉MacLaughlin, J A -- Anderson, R R -- Holick, M F -- AM 27334/AM/NIADDK NIH HHS/ -- New York, N.Y. -- Science. 1982 May 28;216(4549):1001-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6281884" target="_blank"〉PubMed〈/a〉
    Keywords: Cholecalciferol/*biosynthesis/metabolism ; Dehydrocholesterols/radiation effects ; Ergosterol/metabolism ; Humans ; In Vitro Techniques ; Isomerism ; Photochemistry ; Skin/*metabolism ; Spectrum Analysis ; Structure-Activity Relationship ; Ultraviolet Rays
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    Oxytocin induces maternal behavior in virgin female rats (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-05-07
    Description: Intracerebroventricular administration of oxytocin to virgin female rats that had been ovariectomized and primed with estrogen 48 hours previously induced a rapid onset of full maternal behavior. The maternal behavior persisted and its incidence was dose-related. Tocinoic acid, the ring structure of oxytocin, also rapidly induced the onset of persistent, full maternal behavior. Arginine vasopressin induced persistent maternal behavior, but this behavior had a later onset. Prostaglandin F2 alpha induced strong partial maternal behavior, which showed early onset but did not persist. Many other peptides, ovarian steroids, and prostaglandin E2 were no more effective than saline. These findings suggest that the release of oxytocin and prostaglandin F2 alpha during labor may promote maternal behavior in rats.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Pedersen, C A -- Ascher, J A -- Monroe, Y L -- Prange, A J Jr -- MH-22536/MH/NIMH NIH HHS/ -- MH-32316/MH/NIMH NIH HHS/ -- MH-34933/MH/NIMH NIH HHS/ -- New York, N.Y. -- Science. 1982 May 7;216(4546):648-50.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7071605" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Arginine Vasopressin/pharmacology ; Brain/physiology ; Female ; Injections, Intraventricular ; *Maternal Behavior ; Oxytocin/administration & dosage/*pharmacology ; Rats ; Structure-Activity Relationship
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    Translational efficiency of transfer RNA's: uses of an extended anticodon (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-11-12
    Description: Transfer RNA's are probably very strongly selected for translational efficiency. In this article, the argument is presented that the coding performance of the triplet anticodon is enhanced by selection of a matching anticodon loop and stem sequence. the anticodon plus these nearby sequence features (the extended anticodon) therefore contains more coding information than the anticodon alone and can perform more efficiently and accurately at the ribosome. This idea successfully accounts for the relative efficiencies of many transfer RNA's.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Yarus, M -- New York, N.Y. -- Science. 1982 Nov 12;218(4573):646-52.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6753149" target="_blank"〉PubMed〈/a〉
    Keywords: Base Sequence ; Escherichia coli/genetics ; Kinetics ; Nucleic Acid Conformation ; *Protein Biosynthesis ; RNA, Transfer/*genetics ; Ribosomes/metabolism ; Structure-Activity Relationship ; Suppression, Genetic
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    Alcohol and pregnancy (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-09-23
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉New York, N.Y. -- Science. 1983 Sep 23;221(4617):1244-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6684327" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Dose-Response Relationship, Drug ; Ethanol/*adverse effects ; Female ; Pregnancy ; Pregnancy, Animal/*drug effects
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    Platelet thromboxane synthetase inhibitors with low doses of aspirin: possible resolution of the "aspirin dilemma" (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-04-29
    Description: Selective pharmacological inhibition of thromboxane A2 synthesis did not prevent arachidonate-induced aggregation of human platelets in vitro. Prevention was instead achieved by a combination of thromboxane A2 inhibitors with low concentrations of aspirin. The latter partially reduced the proaggregatory cyclooxygenase products that accumulated when thromboxane A2 synthesis was blocked. The aspirin concentrations did not affect per se either platelet aggregation or prostacyclin synthesis in cultured human endothelial cells. The combination of thromboxane synthetase inhibitors with low doses of aspirin may offer greater antithrombotic potential than either drug alone.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Bertele, V -- Falanga, A -- Tomasiak, M -- Dejana, E -- Cerletti, C -- de Gaetano, G -- New York, N.Y. -- Science. 1983 Apr 29;220(4596):517-9.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6682245" target="_blank"〉PubMed〈/a〉
    Keywords: Aspirin/*pharmacology ; Blood Platelets/*drug effects/enzymology ; Dose-Response Relationship, Drug ; Drug Interactions ; Humans ; Imidazoles/pharmacology ; Methacrylates/pharmacology ; Oxidoreductases/*antagonists & inhibitors ; Platelet Aggregation/drug effects ; Thromboxane-A Synthase/*antagonists & inhibitors
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    Bioactive cardiac substances: potent vasorelaxant activity in mammalian atria (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-07-01
    Description: Mammalian atrial extracts possess natriuretic and diuretic activity. In experiments reported here it was found that atrial, but not ventricular, extract also causes relaxation of isolated vascular and nonvascular smooth muscle preparations. The smooth muscle relaxant activity of atrial extract was heat-stable and concentration-dependent and could be destroyed with protease. Rabbit aortic and chick rectum strips were used for the detection of atrial biological activity. The atrial activity was separated by column chromatography into two peaks having apparent molecular weights of 20,000 to 30,000 and less than 10,000. The atrial substance that copurified with the smooth muscle relaxant activity in both peaks caused natriuresis when injected into conscious rats. It appears that atria possess at least two peptides that elicit smooth muscle relaxation and natriuresis, suggesting an endogenous system of fluid volume regulation.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Currie, M G -- Geller, D M -- Cole, B R -- Boylan, J G -- YuSheng, W -- Holmberg, S W -- Needleman, P -- New York, N.Y. -- Science. 1983 Jul 1;221(4605):71-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6857267" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; *Atrial Function ; Chickens ; Chromatography, Gel ; Dogs ; Dose-Response Relationship, Drug ; Humans ; Molecular Weight ; Muscle, Smooth/drug effects ; Muscle, Smooth, Vascular/*drug effects ; Natriuresis/drug effects ; Rabbits ; Rats ; Swine ; Vasodilation/drug effects
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    Drug history modifies the behavioral effects of pentobarbital (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-04-15
    Description: Behavior of squirrel monkeys, maintained by the termination of stimuli associated with electric shock, was suppressed by response-dependent shock delivery. The effects of pentobarbital on this behavior depended on whether monkeys had previously received morphine. In monkeys without experience with drugs, pentobarbital increased responding. In monkeys with recent experience with morphine, however, pentobarbital resulted in a smaller increase or decrease in responding. The rate-decreasing effects of pentobarbital after a history of morphine administration could be reversed by the administration of d-amphetamine. These findings suggest that the behavioral effects of abused drugs may depend on previous experience with other drugs, even when those drugs are from a different pharmacological class.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Glowa, J R -- Barrett, J E -- DA 02658/DA/NIDA NIH HHS/ -- DA 02873/DA/NIDA NIH HHS/ -- MH 07658/MH/NIMH NIH HHS/ -- etc. -- New York, N.Y. -- Science. 1983 Apr 15;220(4594):333-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6682244" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Behavior, Animal/*drug effects ; Dextroamphetamine/pharmacology ; Dose-Response Relationship, Drug ; Drug Interactions ; Humans ; Macaca mulatta ; Male ; Morphine/pharmacology ; Pentobarbital/*pharmacology ; Saimiri ; Substance-Related Disorders/physiopathology
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    The thymus-adrenal connection: thymosin has corticotropin-releasing activity in primates (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-12-23
    Description: Endotoxin-free thymosin fraction 5 elevated corticotropin, beta-endorphin, and cortisol in a dose- and time-dependent fashion when administered intravenously to prepubertal cynomolgus monkeys. Two synthetic component peptides of thymosin fraction 5 had no acute effects on pituitary function, suggesting that some other peptides in thymosin fraction 5 were responsible for its corticotropin-releasing activity. In agreement with these observations, total thymectomy of juvenile macaques was associated with decreases in plasma cortisol, corticotropin, and beta-endorphin. These findings indicate that the prepubertal primate thymus contains corticotropin-releasing activity that may contribute to a physiological immunoregulatory circuit between the developing immunological and pituitary-adrenal systems.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Healy, D L -- Hodgen, G D -- Schulte, H M -- Chrousos, G P -- Loriaux, D L -- Hall, N R -- Goldstein, A L -- CA 24974/CA/NCI NIH HHS/ -- New York, N.Y. -- Science. 1983 Dec 23;222(4630):1353-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6318312" target="_blank"〉PubMed〈/a〉
    Keywords: Adrenocorticotropic Hormone/*blood ; Animals ; Dose-Response Relationship, Drug ; Endorphins/blood ; Female ; Hydrocortisone/blood ; Kinetics ; Macaca fascicularis ; Thymectomy ; Thymosin/analogs & derivatives/*pharmacology ; Thymus Gland/*physiology ; beta-Endorphin
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    Implication of nonlinear kinetics on risk estimation in carcinogenesis (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-03-04
    Description: Efforts in estimating carcinogenic risk in humans from long-term exposure to chemical carcinogens have centered on the problem of low-dose extrapolation. For chemicals with metabolites that interact with DNA, it may be more meaningful to relate tumor response to the concentration of the DNA adducts in the target organ rather than to the applied dose. Many data suggest that the relation between tumor response and concentration of DNA adducts in the target organ may be linear. This implies that the nonlinearities of the dose-response curve for tumor induction may be due to the kinetic processes involved in the formation of carcinogen metabolite--DNA adducts. Of particular importance is the possibility that the kinetic processes may show a nonlinear "hockey-stick" like behavior which results from saturation of detoxification or DNA repair processes. The mathematical models typically used for low-dose extrapolation are shown potentially to overestimate risk by several orders of magnitude when nonlinear kinetics are present.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Hoel, D G -- Kaplan, N L -- Anderson, M W -- New York, N.Y. -- Science. 1983 Mar 4;219(4588):1032-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6823565" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Carcinogens/*administration & dosage ; Cell Transformation, Neoplastic/*drug effects ; DNA, Neoplasm/genetics ; Dose-Response Relationship, Drug ; Humans ; Kinetics ; Models, Biological ; Neoplasms/*chemically induced ; Risk
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    A parathyroid hormone inhibitor in vivo: design and biological evaluation of a hormone analog (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-06-03
    Description: A synthetic analog of bovine parathyroid hormone (bPTH), [tyrosine-34] bPTH-(7-34)NH2, was found to inhibit parathyroid hormone action in vivo. When the analog and parathyroid hormone were infused simultaneously to rats at a molar ratio of 200 to 1, the analog inhibited the excretion of urinary phosphate and adenosine 3',5'-monophosphate. When infused alone at the same dose rate, the analog was devoid of agonist activity. The compound was prepared by following design principles developed for inhibitors of parathyroid hormone, and is believed to be the first antagonist of parathyroid hormone that is effective in vivo.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Horiuchi, N -- Holick, M F -- Potts, J T Jr -- Rosenblatt, M -- AM11749/AM/NIADDK NIH HHS/ -- New York, N.Y. -- Science. 1983 Jun 3;220(4601):1053-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6302844" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Animals ; Cyclic AMP/urine ; Dose-Response Relationship, Drug ; Male ; Parathyroid Hormone/*antagonists & inhibitors/*pharmacology ; Peptide Fragments/*pharmacology ; Phosphates/urine ; Rats
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    Fragile sites in chromosomes: possible model for the study of spontaneous chromosome breakage (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-04-01
    Description: The tissue culture condition that is required for the type of chromosome breakage seen at most fragile sites, namely, the absence of folic acid and thymidine in the medium, greatly enhanced micronucleus formation in proliferating lymphocyte cultures from normal individuals. This suggests that chromosome breakage at fragile sites and the apparently spontaneous damage that gives rise to micronuclei are controlled by the same mechanism.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Jacky, P B -- Beek, B -- Sutherland, G R -- New York, N.Y. -- Science. 1983 Apr 1;220(4592):69-70.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6828880" target="_blank"〉PubMed〈/a〉
    Keywords: Adolescent ; Adult ; Cell Nucleus/drug effects/ultrastructure ; Cells, Cultured ; Child ; *Chromosome Aberrations ; Chromosome Fragile Sites ; *Chromosome Fragility ; Culture Media ; Dose-Response Relationship, Drug ; Female ; Folic Acid/pharmacology ; Humans ; Lymphocytes/ultrastructure ; Male ; Middle Aged ; Thymidine/pharmacology
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    Z-DNA moves toward "real biology" (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-11-04
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Kolata, G -- New York, N.Y. -- Science. 1983 Nov 4;222(4623):495-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6623088" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; *Dna ; Eukaryota/genetics ; Humans ; *Nucleic Acid Conformation ; Species Specificity ; Structure-Activity Relationship
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    Inhibition of gastric acid secretion in rats by intracerebral injection of corticotropin-releasing factor (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-11-25
    Description: Intracisternal injection of ovine corticotropin-releasing factor (CRF) into the pylorus-ligated rat or the rat with gastric fistula resulted in a dose-dependent inhibition of gastric secretion stimulated with pentagastrin or thyrotropin-releasing hormone. When injected into the lateral hypothalamus--but not when injected into the cerebral cortex--CRF suppressed pentagastrin-stimulated acid secretion. The inhibitory effect of CRF was blocked by vagotomy and adrenalectomy but not by hypophysectomy or naloxone treatment. These results indicate that CRF acts within the brain to inhibit gastric acid secretion through vagal and adrenal mechanisms and not through hypophysiotropic effects.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Tache, Y -- Goto, Y -- Gunion, M W -- Vale, W -- River, J -- Brown, M -- AM30110/AM/NIADDK NIH HHS/ -- New York, N.Y. -- Science. 1983 Nov 25;222(4626):935-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6415815" target="_blank"〉PubMed〈/a〉
    Keywords: Adrenalectomy ; Animals ; Brain/*drug effects ; Cerebral Cortex/drug effects ; Corticotropin-Releasing Hormone/administration & dosage/*pharmacology ; Dose-Response Relationship, Drug ; Gastric Acid/*secretion ; Hypophysectomy ; Hypothalamus/drug effects ; Male ; Pentagastrin/antagonists & inhibitors ; Rats ; Rats, Inbred Strains ; Thyrotropin-Releasing Hormone/antagonists & inhibitors ; Vagotomy
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    Antibodies that react with predetermined sites on proteins (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-02-11
    Description: Contrary to previous predictions, relatively short synthetic peptides that mimic part of a protein sequence are routinely capable of eliciting an antiserum that reacts with the partially mimicked protein. Peptides capable of eliciting protein-reactive serums are frequently represented in the primary sequence of a protein, can be characterized by a set of simple chemical rules, and are confined neither to immunodominant regions of intact proteins nor to the amino or carboxyl terminals. As such, synthetic peptide immunogens are valuable for eliciting reagents with predetermined specificity that can be used for basic research. In addition, some synthetic peptides are capable of mimicking regions of virus proteins and eliciting immune responses in animals that are protective against the viral agents. Such peptides may thus serve as the basis for safe, chemically defined synthetic vaccines.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Sutcliffe, J G -- Shinnick, T M -- Green, N -- Lerner, R A -- R01 AI 18509/AI/NIAID NIH HHS/ -- New York, N.Y. -- Science. 1983 Feb 11;219(4585):660-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6186024" target="_blank"〉PubMed〈/a〉
    Keywords: *Antibody Specificity ; Cross Reactions ; *Epitopes ; Peptides/immunology ; Proteins/*immunology ; Structure-Activity Relationship ; Vaccines/immunology
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    Monoclonal antibodies reveal the structural basis of antibody diversity (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-11-18
    Description: Hybridoma technology has made it possible to introduce into continuous culture normal antibody-forming cells and to obtain large amounts of the immunoglobulin produced by each of these cells. Examination of the structure of a number of monoclonal antibodies that react with a single antigen has provided new information on the structural basis of the specificity and affinity of antibodies. Comparisons of families of monoclonal antibodies derived from a single germ line gene revealed the importance of somatic mutation in generating antibody diversity. Monoclonal antibodies that react with variable regions of other monoclonals allow the further dissection and modulation of the immune response. Finally, the continued somatic instability of immunoglobulin genes in cultured antibody-forming cells makes it possible to determine the rate of somatic mutation and to generate mutant monoclonal antibodies that may be more effective serological reagents.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Teillaud, J L -- Desaymard, C -- Giusti, A M -- Haseltine, B -- Pollock, R R -- Yelton, D E -- Zack, D J -- Scharff, M D -- 5T32GM7288/GM/NIGMS NIH HHS/ -- AI05231/AI/NIAID NIH HHS/ -- AI10702/AI/NIAID NIH HHS/ -- New York, N.Y. -- Science. 1983 Nov 18;222(4625):721-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6356353" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Animals ; Antibodies, Monoclonal/genetics/*immunology ; *Antibody Diversity ; Antibody Specificity ; Genes ; Hybridomas/immunology ; Immunoglobulin Idiotypes/immunology ; Immunoglobulin Variable Region/genetics ; Mice ; Mutation ; Protein Conformation ; Structure-Activity Relationship
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    Benzoquinolinediones: activity as insect teratogens (1983)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1983-10-28
    Description: Morphological abnormalities including extra compound eyes, extra heads, and distally duplicated legs were generated in cricket embryos by treating eggs with single doses of either benz[g]isoquinoline-5,10-dione or benzo[h]quinoline-5,6-dione. Slight structural modifications of the molecules resulted in a loss of teratogenic activity, although embryotoxicity occurred. These potent insect teratogens can be used for analysis of developmental events during embryogenesis.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Walton, B T -- Ho, C -- Ma, C Y -- O'Neill, E G -- Kao, G L -- New York, N.Y. -- Science. 1983 Oct 28;222(4622):422-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6623081" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Isoquinolines/*toxicity ; Orthoptera/*embryology ; Quinolines/*toxicity ; *Quinolones ; Structure-Activity Relationship ; *Teratogens
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    Criteria for evidence of chemical carcinogenicity. Interdisciplinary Panel on Carcinogenicity (1984)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1984-08-17
    Description: The Interdisciplinary Panel on Carcinogenicity reviewed and reevaluated criteria for assessing evidence of carcinogenicity of chemical substances. The panel reviewed criteria applicable to data derived from human epidemiological studies and from both in vivo and in vitro laboratory studies. A critical appraisal of all these sources of information led to the conclusion that the characterization of human risk always requires interdisciplinary evaluation of the entire array of data on a case-by-case basis. Animal studies, whenever possible, should be augmented by studies of mechanisms, metabolism, and pharmacodynamics. Such studies may assist in assessing risk to man. Recognizing the utility of such data should point the way for better assessment in the future.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉New York, N.Y. -- Science. 1984 Aug 17;225(4663):682-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6463646" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Biological Assay ; *Carcinogens/metabolism/pharmacology ; Carcinogens, Environmental ; Cell Transformation, Neoplastic ; Dose-Response Relationship, Drug ; Environmental Exposure ; Epidemiologic Methods ; Humans ; In Vitro Techniques ; Mixed Function Oxygenases/metabolism ; Mutagenicity Tests ; Neoplasms/chemically induced ; Risk ; Time Factors ; United States
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    Inhibition of dihydropteridine reductase by novel 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine analogs (1984)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1984-04-27
    Description: Hydroxylated derivatives of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), a nigrostriatal neurotoxin in humans and primates, noncompetitively inhibited dihydropteridine reductase from human liver and rat striatal synaptosomes in vitro at micromolar concentrations. In contrast, MPTP and its chloro- and norderivatives did not inhibit this enzyme at lower than millimolar concentrations. Dihydropteridine reductase converts dihydrobiopterin to tetrahydrobiopterin, the required cofactor for the hydroxylation of aromatic amino acids during the synthesis of dopamine and serotonin.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Abell, C W -- Shen, R S -- Gessner, W -- Brossi, A -- HD 14635/HD/NICHD NIH HHS/ -- New York, N.Y. -- Science. 1984 Apr 27;224(4647):405-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6608790" target="_blank"〉PubMed〈/a〉
    Keywords: 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine ; Animals ; Corpus Striatum/enzymology ; Dihydropteridine Reductase/*antagonists & inhibitors ; Humans ; Hydroxylation ; Liver/enzymology ; NAD/metabolism ; NADH, NADPH Oxidoreductases/*antagonists & inhibitors ; Pyridines/*pharmacology ; Rats ; Structure-Activity Relationship ; Synaptosomes/enzymology
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  • 53
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    Nucleotide sequence of a human Blym transforming gene activated in a Burkitt's lymphoma (1984)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1984-08-03
    Description: The nucleotide sequence of a human Blym-1 transforming gene activated in a Burkitt's lymphoma cell line was determined. This sequence predicts a small protein of 58 amino acids that is 33 percent identical to the predicted product of chicken Blym-1, the activated transforming gene of chicken B cell lymphomas. Both the human and chicken Blym-1 genes exhibit significant identity to an amino-terminal region of transferrins.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Diamond, A -- Devine, J M -- Cooper, G M -- CA 07250/CA/NCI NIH HHS/ -- CA 28946/CA/NCI NIH HHS/ -- New York, N.Y. -- Science. 1984 Aug 3;225(4661):516-9.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6330897" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Base Sequence ; Burkitt Lymphoma/*genetics ; Cell Line ; *Cell Transformation, Neoplastic ; DNA Restriction Enzymes ; Humans ; *Oncogenes ; Structure-Activity Relationship ; Transcription, Genetic ; Transferrin/genetics
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    Activation of antitumor agent gilvocarcins by visible light (1984)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1984-01-06
    Description: Gilvocarcins that are antitumor agents are activated by low doses of visible light to induce bacteriophage lambda in Escherichia coli. This result is dependent on interaction with DNA. Gilvocarcin M, an analog without antitumor activity, failed to induce the prophage after light exposure, thus demonstrating a correlation between photosensitizing and antitumor activities. These results raise several possibilities regarding the mode of action of gilvocarcins as antitumor agents in vivo, involving light or enzymatic activating systems, which could be exploited in human cancer therapy.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Elespuru, R K -- Gonda, S K -- New York, N.Y. -- Science. 1984 Jan 6;223(4631):69-71.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6229029" target="_blank"〉PubMed〈/a〉
    Keywords: *Aminoglycosides ; *Anti-Bacterial Agents ; Antibiotics, Antineoplastic/*pharmacology/radiation effects ; Bacteriophage lambda/growth & development ; Benzopyrans ; Coumarins ; Glycosides/pharmacology/radiation effects ; *Light ; Methoxsalen/pharmacology ; Structure-Activity Relationship ; Trioxsalen/pharmacology ; Ultraviolet Rays ; Virus Activation/*drug effects
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    Amphiphilic secondary structure: design of peptide hormones (1984)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1984-01-20
    Description: Peptide synthesis can be used for elucidating the roles of secondary structures in the specificity of hormones, antigens, and toxins. Intermediate sized peptides with these activities assume amphiphilic secondary structures in the presence of membranes. When models are designed to optimize the amphiphilicity of the secondary structure, stronger interactions can be observed with the synthetic peptides than with the naturally occurring analogs.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Kaiser, E T -- Kezdy, F J -- HL-18577/HL/NHLBI NIH HHS/ -- New York, N.Y. -- Science. 1984 Jan 20;223(4633):249-55.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6322295" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Apolipoprotein A-I ; Apolipoproteins ; Binding Sites ; Calcitonin ; Chemical Phenomena ; Chemistry ; Corticotropin-Releasing Hormone ; Endorphins ; Glucagon ; Growth Hormone-Releasing Hormone ; *Hormones/pharmacology ; Lipoproteins, HDL ; Melitten ; Models, Structural ; *Peptides/chemical synthesis/metabolism/pharmacology ; Protein Conformation ; Structure-Activity Relationship ; beta-Endorphin
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    A model study of fecapentaenes: mutagens of bacterial origin with alkylating properties (1984)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1984-08-03
    Description: Fecapentaene-14 and -12 are directly acting mutagens that do not require metabolic activation. Their unusual structure suggests a possible mechanism of action. A carbocation that is formed by the addition of an electrophilic species (such as a proton) to the enol ether is most probably the reactive species. A series of model enol ethers with conjugated systems of various lengths was prepared, and a correlation between mutagenicity and increasing reactivity of derived carbocations was found. The glycerol moiety does not play a crucial role in the overall reactivity of the fecapentaenes.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Gupta, I -- Suzuki, K -- Bruce, R W -- Krepinsky, J J -- Yates, P -- New York, N.Y. -- Science. 1984 Aug 3;225(4661):521-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6377497" target="_blank"〉PubMed〈/a〉
    Keywords: *Alkylating Agents ; Mutagenicity Tests ; Mutagens/*toxicity ; *Mutation ; Polyenes/toxicity ; Salmonella typhimurium/drug effects ; Structure-Activity Relationship
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    Inhibitors of poly(adenosine diphosphate-ribose) synthesis: effect on other metabolic processes (1984)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1984-02-10
    Description: 3-Aminobenzamide and benzamide, purported to be specific inhibitors of the synthesis of poly(adenosine diphosphate-ribose), were used to elucidate possible functions of this biopolymer. These compounds, at frequently used experimental concentrations, not only inhibited the action of poly(adenosine diphosphate-ribose) synthetase but also affected cell viability, glucose metabolism, and DNA synthesis. Thus, the usefulness of 3-aminobenzamide and benzamide may be severely restricted by the difficulty of finding a dose small enough to inhibit the synthetase without producing additional metabolic effects.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Milam, K M -- Cleaver, J E -- New York, N.Y. -- Science. 1984 Feb 10;223(4636):589-91.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6420886" target="_blank"〉PubMed〈/a〉
    Keywords: Benzamides/*toxicity ; Cell Line ; DNA Replication/drug effects ; Humans ; Kinetics ; Lymphocytes ; Nucleoside Diphosphate Sugars/*biosynthesis ; Poly Adenosine Diphosphate Ribose/*biosynthesis ; Poly(ADP-ribose) Polymerases/metabolism ; Structure-Activity Relationship
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    Carbocyclic arabinofuranosyladenine (cyclaradine): efficacy against genital herpes in guinea pigs (1983)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1983-09-30
    Description: Carbocyclic arabinofuranosyladenine (cyclaradine), a novel nucleoside analog with such desired features as hydrolytic and enzymatic stability, adenosine deaminase resistance, and low systemic toxicity, inhibited the replication of herpes simplex virus types 1 and 2. The 5'-methoxyacetate prodrug form exhibited significant efficacy in the topical treatment of genital infections by herpes simplex virus type 2.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Vince, R -- Daluge, S -- Lee, H -- Shannon, W M -- Arnett, G -- Schafer, T W -- Nagabhushan, T L -- Reichert, P -- Tsai, H -- CA 23263/CA/NCI NIH HHS/ -- New York, N.Y. -- Science. 1983 Sep 30;221(4618):1405-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6684328" target="_blank"〉PubMed〈/a〉
    Keywords: Acyclovir/therapeutic use ; Animals ; Disease Models, Animal ; Female ; Guinea Pigs ; Herpes Genitalis/*drug therapy ; Male ; Structure-Activity Relationship ; Vidarabine/*analogs & derivatives/therapeutic use
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  • 59
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    Opioid peptides mediate the suppressive effect of stress on natural killer cell cytotoxicity (1984)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1984-01-13
    Description: The cytotoxic activity of natural killer cells was investigated in rats subjected to one of two inescapable footshock stress paradigms, both of which induce analgesia, but only one via activation of opioid mechanisms. Splenic natural killer cell activity was suppressed by the opioid, but not the nonopioid, form of stress. This suppression was blocked by the opioid antagonist naltrexone. Similar suppression of natural killer activity was induced by high doses of morphine. These results suggest that endogenous opioid peptides mediate the suppressive effect of certain forms of stress on natural killer cell cytotoxicity.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Shavit, Y -- Lewis, J W -- Terman, G W -- Gale, R P -- Liebeskind, J C -- MH15795/MH/NIMH NIH HHS/ -- NS07628/NS/NINDS NIH HHS/ -- New York, N.Y. -- Science. 1984 Jan 13;223(4632):188-90.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6691146" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; *Cytotoxicity, Immunologic/drug effects ; Dose-Response Relationship, Drug ; Endorphins/*physiology ; Female ; Killer Cells, Natural/*immunology ; Morphine/*pharmacology ; Naltrexone/pharmacology ; Rats ; Rats, Inbred F344 ; Stress, Physiological/*immunology
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    Nicarbazin complex yields dinitrocarbanilide as ultrafine crystals with improved anticoccidial activity (1983)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1983-11-11
    Description: Nicarbazin, a drug used to control the protozoal disease coccidiosis in poultry, is a complex of the highly insoluble drug 4,4'-dinitrocarbanilide with 2-hydroxy-4,6-dimethylpyrimidine. The structures of this and other 4,4'-dinitrocarbanilide complexes have not been determined, but an analogous 2:1 complex of 4,4'-dinitrodiphenylamine with 1,4-diacetylpiperazine has been prepared in which the only possible bonds are hydrogen bonds between the amide carbonyls and amino hydrogens. Scanning electron microscopy revealed that micron-size crystals of nicarbazin disintegrate in water to form much smaller dinitrocarbanilide crystals. Similar complex dissolution in the gut of poultry may account for the greater effectiveness of dinitrocarbanilide when administered as complexed rather than uncomplexed drug. Particle size problems associated with other highly insoluble drugs and pesticides may be resolved by the use of nicarbazin-like complexes.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Rogers, E F -- Brown, R D -- Brown, J E -- Kazazis, D M -- Leanza, W J -- Nichols, J R -- Ostlind, D A -- Rodino, T M -- New York, N.Y. -- Science. 1983 Nov 11;222(4624):630-2.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6635662" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Carbanilides/*administration & dosage ; Chickens ; Coccidiostats ; Crystallization ; Intestinal Absorption ; Nicarbazin/*administration & dosage ; Poultry Diseases/*prevention & control ; Solubility ; Structure-Activity Relationship
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    Insect prothoracicotropic hormone: evidence for two molecular forms (1984)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1984-06-15
    Description: In an insect, the tobacco hornworm Manduca sexta, the cerebral neuropeptide prothoracicotropic hormone (PTTH), the primary effector of postembryonic development, exists as two molecular forms. These two PTTH's elicit characteristic in vitro dose responses of activation of prothoracic glands from different developmental stages, an indication that during development the glands change in their sensitivity to the neurohormones. Both PTTH's are active in a specific in situ bioassay. Since they may be released in situ at stage-specific times to evoke distinctly different developmental responses, the PTTH neuroendocrine axis appears to be an effective system for determining the functions of molecular forms of a neurohormone in the regulation of growth and development.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Bollenbacher, W E -- Katahira, E J -- O'Brien, M -- Gilbert, L I -- Thomas, M K -- Agui, N -- Baumhover, A H -- AM-30118/AM/NIADDK NIH HHS/ -- AM-31642/AM/NIADDK NIH HHS/ -- NS-18791/NS/NINDS NIH HHS/ -- New York, N.Y. -- Science. 1984 Jun 15;224(4654):1243-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6732895" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Biological Assay ; Bombyx ; Chromatography, Gel ; Dose-Response Relationship, Drug ; Insect Hormones/pharmacology/*physiology ; Insects/drug effects/growth & development/physiology ; Isoelectric Focusing ; Larva
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    Bromine residue at hydrophilic region influences biological activity of aplysiatoxin, a tumor promoter (1983)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1983-12-16
    Description: Aplysiatoxin and debromoaplysiatoxin, which are isolated from the seaweed, Lyngbya gracilis, differ in their chemical structure only by the presence or absence of a bromine residue in the hydrophilic region. The function and the structure-activity relation of the hydrophilic region are not known. Aplysiatoxin increased malignant transformation, stimulated DNA synthesis, and inhibited the binding of phorbol-12,13-dibutyrate and epidermal growth factor to cell receptors. Debromoaplysiatoxin inhibited the binding of these two substances as strongly as aplysiatoxin but did not increase malignant transformation or stimulate DNA synthesis. These results indicate that a slight change in the chemical structure of the hydrophilic region of aplysiatoxin affects its abilities to increase cell transformation and stimulate DNA synthesis and that the abilities of the tumor promoters to inhibit the binding of phorbol-12,13-dibutyrate and epidermal growth factor are dissociable from their abilities to increase cell transformation and stimulate DNA synthesis under some circumstances.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Shimomura, K -- Mullinix, M G -- Kakunaga, T -- Fujiki, H -- Sugimura, T -- New York, N.Y. -- Science. 1983 Dec 16;222(4629):1242-4.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6316505" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; *Caenorhabditis elegans Proteins ; Carcinogens/*pharmacology ; Carrier Proteins ; Cell Line ; Cell Transformation, Neoplastic/*drug effects ; Chemical Phenomena ; Chemistry ; DNA/biosynthesis ; Epidermal Growth Factor/metabolism ; Lactones/analysis/*pharmacology ; *Lyngbya Toxins ; Mice ; Phorbol 12,13-Dibutyrate ; Phorbol Esters/metabolism ; *Protein Kinase C ; Receptor, Epidermal Growth Factor ; Receptors, Cell Surface/metabolism ; *Receptors, Drug ; Structure-Activity Relationship
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    Potentiation of bleomycin lethality by anticalmodulin drugs: a role for calmodulin in DNA repair (1984)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1984-06-22
    Description: Treatment of exponentially growing Chinese hamster ovary cells with bleomycin causes a dose-dependent decrease in cell survival due to DNA damage. This lethal effect can be potentiated by the addition of a nonlethal dose of the anticalmodulin drug N-(4-aminobutyl)-5-chloro-2-naphthalenesulfonamide ( W13 ) but not its inactive analog N-(4-aminobutyl)-2-naphthalenesulfonamide ( W12 ). By preventing the repair of damaged DNA, W13 also inhibits recovery from potentially lethal damage induced by bleomycin. These data suggest a role for calmodulin in the DNA repair pathway.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Chafouleas, J G -- Bolton, W E -- Means, A R -- RR-05425/RR/NCRR NIH HHS/ -- New York, N.Y. -- Science. 1984 Jun 22;224(4655):1346-8.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6203171" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Bleomycin/*pharmacology ; Calmodulin/*antagonists & inhibitors/*physiology ; Cell Division/drug effects ; Cell Line ; Cell Survival/drug effects ; Cricetinae ; Cricetulus ; DNA Repair/*drug effects ; Dose-Response Relationship, Drug ; Drug Synergism ; Sulfonamides/pharmacology
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    Amiloride directly inhibits the Na,K-ATPase activity of rabbit kidney proximal tubules (1983)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1983-05-27
    Description: Amiloride inhibited the ouabain-sensitive rate of oxygen consumption (QO2) of a suspension of rabbit intact proximal tubules in the presence of different concentrations of extracellular sodium. Measurements of the ouabain-sensitive QO2 in the presence of nystatin, the tissue sodium and potassium contents of the tubules in suspension, and the sodium- and potassium-dependent adenosinetriphosphatase (Na,K-ATPase) activity of lysed tubule membranes indicated that the effect of amiloride was due to a direct inhibition of the Na,K-ATPase activity of the proximal tubule.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Soltoff, S P -- Mandel, L J -- AM26816/AM/NIADDK NIH HHS/ -- GM29256/GM/NIGMS NIH HHS/ -- New York, N.Y. -- Science. 1983 May 27;220(4600):957-8.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6302840" target="_blank"〉PubMed〈/a〉
    Keywords: Amiloride/*pharmacology ; Animals ; Dose-Response Relationship, Drug ; Female ; Ion Channels/drug effects ; Kidney Tubules, Proximal/drug effects/*enzymology ; Nystatin/pharmacology ; Ouabain/pharmacology ; Oxygen Consumption/drug effects ; Pyrazines/*pharmacology ; Rabbits ; Rats ; Sodium/metabolism ; Sodium-Potassium-Exchanging ATPase/*antagonists & inhibitors/metabolism
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    Rat transforming growth factor type 1: structure and relation to epidermal growth factor (1984)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1984-03-09
    Description: The complete amino acid sequence of rat transforming growth factor type 1 has been determined. This growth factor, obtained from retrovirus-transformed fibroblasts, is structurally and functionally related to mouse epidermal growth factor and human urogastrone. Production of this polypeptide by various neoplastic cells might contribute to the continued expression of the transformed phenotype.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Marquardt, H -- Hunkapiller, M W -- Hood, L E -- Todaro, G J -- New York, N.Y. -- Science. 1984 Mar 9;223(4640):1079-82.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6320373" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Animals ; Cell Line ; *Cell Transformation, Neoplastic ; DNA/biosynthesis ; Epidermal Growth Factor/*metabolism/pharmacology ; Humans ; Idoxuridine/metabolism ; Mice ; Peptide Biosynthesis ; Peptides/*metabolism/pharmacology ; Rats ; Receptor, Epidermal Growth Factor ; Receptors, Cell Surface/metabolism ; Structure-Activity Relationship ; Transforming Growth Factors
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    Need a catalyst? Design an enzyme (1984)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1984-01-20
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Maugh, T H 2nd -- New York, N.Y. -- Science. 1984 Jan 20;223(4633):269-71.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6608147" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Binding Sites ; Biochemistry/*methods ; Catalysis ; *Cloning, Molecular ; Enzymes/genetics/*metabolism ; Mutation ; Structure-Activity Relationship ; Substrate Specificity ; Tetrahydrofolate Dehydrogenase/metabolism ; Tyrosine-tRNA Ligase/metabolism ; beta-Lactamases/metabolism
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    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 67
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    A potential second messenger role for unsaturated fatty acids: activation of Ca2+-dependent protein kinase (1984)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1984-05-11
    Description: Arachidonate and other unsaturated long-chain fatty acids were found to activate protein kinase C from human neutrophils. Kinase activation by arachidonate required calcium and was enhanced by diolein but did not require exogenous phosphatidylserine. Submaximal levels of arachidonate also enhanced the affinity of the kinase for calcium during activation by phosphatidylserine. Thus the release of arachidonate, which is triggered in many cell types by ligand-receptor interactions, could play a second messenger role in the regulation of cellular function by activation of protein kinase C.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉McPhail, L C -- Clayton, C C -- Snyderman, R -- 5PO1CA29589/CA/NCI NIH HHS/ -- 5RO-1DEO3738/DE/NIDCR NIH HHS/ -- New York, N.Y. -- Science. 1984 May 11;224(4649):622-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6231726" target="_blank"〉PubMed〈/a〉
    Keywords: Arachidonic Acid ; Arachidonic Acids/pharmacology ; Dose-Response Relationship, Drug ; Enzyme Activation ; Fatty Acids, Unsaturated/pharmacology/*physiology ; Humans ; Kinetics ; Neutrophils/enzymology ; Phosphatidylserines/pharmacology ; Protein Kinase C ; Protein Kinases/*metabolism
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  • 68
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    Kainic acid induces sprouting of retinal neurons (1984)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1984-02-03
    Description: The neurotoxin kainic acid caused dose-dependent morphological changes in horizontal cells of the retinas of adult cats and rabbits. High concentrations of kainic acid killed the cells, but when exposed to sublethal doses they contracted their dendritic fields and sent sprouting processes into the inner retina. It appears that kainic acid can induce neuronal growth as well as degeneration and that the potential for morphological plasticity is still present in neurons of the adult mammalian retina.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Peichl, L -- Bolz, J -- New York, N.Y. -- Science. 1984 Feb 3;223(4635):503-4.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6691162" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cats ; Dendrites/ultrastructure ; Dose-Response Relationship, Drug ; Kainic Acid/*pharmacology ; Nerve Degeneration/drug effects ; Neurons/cytology/*drug effects ; Pyrrolidines/*pharmacology ; Rabbits ; Retina/cytology/*drug effects
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  • 69
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    Interchangeability of stress and amphetamine in sensitization (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-01-18
    Description: In view of similarities between the behavioral, biochemical, and electrophysiological effects of amphetamine and stress, we tested the hypothesis that presentation of a stressor, mild tail pressure, can sensitize an animal to the later effects of amphetamine, and vice versa. Our findings supported this hypothesis and suggest that amphetamine and at least some stressors may be interchangeable in their ability to induce a sensitization. The data raise the possibility that stress might be a common variable contributing to both amphetamine psychosis and some forms of schizophrenia.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Antelman, S M -- Eichler, A J -- Black, C A -- Kocan, D -- New York, N.Y. -- Science. 1980 Jan 18;207(4428):329-31.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7188649" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Behavior, Animal/drug effects/*physiology ; Dextroamphetamine/*pharmacology ; Dopamine/physiology ; Dose-Response Relationship, Drug ; Haloperidol/pharmacology ; Humans ; Male ; Rats ; Schizophrenia/physiopathology ; Stereotyped Behavior/drug effects ; Stress, Physiological/*physiopathology
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  • 70
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    Excitatory and inhibitory effects of serotonin on sensorimotor reactivity measured with acoustic startle (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-07-25
    Description: Serotonin infused into the lateral ventricle in rats produced a dose-dependent depression of the acoustic startle reflex. When infused onto the spinal cord, serotonin produced a dose-dependent increase in startle. Thus the same neurotransmitter can modulate the same behavior in opposite ways, depending on which part of the central nervous system is involved.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Davis, M -- Strachan, D I -- Kass, E -- New York, N.Y. -- Science. 1980 Jul 25;209(4455):521-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7394520" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Dose-Response Relationship, Drug ; Kinetics ; Male ; Rats ; Reflex, Acoustic/*drug effects ; Reflex, Startle/*drug effects ; Serotonin/*pharmacology
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  • 71
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    Endorphin-mediated increases in pain threshold during pregnancy (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-10-10
    Description: Maternal pain thresholds in rats were determined during various stages of pregnancy and parturition by measuring the intensity of electric shock that elicited reflexive jumping. There was a gradual rise in the pain threshold between 16 and 4 days prior to parturition and a more abrupt rise 1 to 2 days before that event. This increase was abolished by long-term administration of the narcotic antagonist naltrexone. The endorphin system is thus an important component of intrinsic mechanisms that modulate responsiveness to aversive stimuli. The data also demonstrate the activation during pregnancy of an endorphin system that is apparently quiescent in nonpregnant female rats treated the same way.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Gintzler, A R -- NIMH GRANT DA01771/DA/NIDA NIH HHS/ -- New York, N.Y. -- Science. 1980 Oct 10;210(4466):193-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7414330" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Dose-Response Relationship, Drug ; Endorphins/antagonists & inhibitors/*physiology ; Female ; Naltrexone/pharmacology ; Pain/*physiopathology ; Pregnancy ; *Pregnancy, Animal ; Rats ; Time Factors
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  • 72
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    Ala-Gly- and Val-Asp-[Arg8]-vasopressin: bovine storage forms of arginine vasopressin with natriuretic activity (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-02-22
    Description: Extracts of fresh-frozen bovine neurohypophysis were purified by chromatographic techniques to isolate and characterize the components that produce natriuresis in nondiuretic dogs. Two compounds with natiuretic properties similar to those of synthetic arginine vasopressin accounted for most of the natriuretic activity and appeared to be the prevalent vasopressin-like molecules in the extract. These peptides were Ala-Gly-[Arg8]-vasopressin and Val-Asp-[Arg8]-vasopressin; the natriuretic potency of each appeared to be similar to synthetic arginine vasopressin and could be observed with doses in the range of 50 picomoles. In the dog the most conspicuous difference between synthetic arginine vasopressin and the new vasopressin peptides was the smaller pressor responses to natriuretic doses of the new compounds.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Gitelman, H J -- Klapper, D G -- Alderman, F R -- Blythe, W B -- New York, N.Y. -- Science. 1980 Feb 22;207(4433):893-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7355269" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Animals ; Arginine Vasopressin/analogs & derivatives/*metabolism/pharmacology ; Biological Assay ; Blood Pressure/drug effects ; Cattle ; Dogs ; Male ; Natriuresis/*drug effects ; Pituitary Gland, Posterior/*metabolism ; Protein Precursors/metabolism ; Structure-Activity Relationship
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    Tumor-promoting phorbol esters stimulate hematopoietic colony formation in vitro (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-04-25
    Description: Tumor-promoting phorbol esters stimulated mouse bone marrow cells to form myeloid colonies in agar cultures without added colony-stimulating factors. The colony-stimulating ability of various phorbol esters correlated well with their ability to promote skin tumors in vivo. These results suggest that phorbol esters mimic the action of specific colony-stimulating factors that regulate growth.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Stuart, R K -- Hamilton, J A -- New York, N.Y. -- Science. 1980 Apr 25;208(4442):402-4.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6245446" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cell Division/drug effects ; Cells, Cultured ; *Colony-Forming Units Assay ; Colony-Stimulating Factors/pharmacology ; Dose-Response Relationship, Drug ; Hematopoietic Stem Cells/*drug effects ; Macrophages/physiology ; Mice ; Monocytes/physiology ; Phorbol Esters/pharmacology ; Phorbols/*pharmacology ; Receptors, Cell Surface/drug effects ; Structure-Activity Relationship ; Tetradecanoylphorbol Acetate/*pharmacology
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  • 74
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    Conversion of 3T3-L1 fibroblasts to fat cells by an inhibitor of methylation: effect of 3-deazaadenosine (1981)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1981-03-13
    Description: 3-Deazaadenosine, an inhibitor of methylation, increased the frequency of conversion of 3T3-L1 fibroblasts to fat cells in a dose-dependent manner. Once converted, the 3T3-L1 fat cells retained their adipose morphology and accumulated triglycerides even when 3-deazaadenosine was removed from the culture medium. 3-Deazaadenosine may perturb cellular methylation and thereby lead to an increase in the frequency of differentiation of 3T3-L1 fibroblasts to fat cells.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Chiang, P K -- New York, N.Y. -- Science. 1981 Mar 13;211(4487):1164-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7466386" target="_blank"〉PubMed〈/a〉
    Keywords: Adipose Tissue/*cytology ; Animals ; Carnitine/pharmacology ; Cell Differentiation/*drug effects ; Cells, Cultured ; Dose-Response Relationship, Drug ; Fibroblasts/cytology ; Methylation ; Mice ; Ribonucleosides/*pharmacology ; Tubercidin/*pharmacology
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    Detection of circulating metallothionein in rats injected with zinc or cadmium (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-11-13
    Description: Circulating metallothionein was measured by radioimmunoassay over a 13-day period in male Sprague-Dawley rats that received a sequence of three intraperitoneal injections (at 3-day intervals) of either 5 milligrams of zinc or 0.8 milligrams of cadmium per kilogram of body weight. These amounts of zinc and cadmium produced metallothionein concentrations in the range of 2 to 5 nanograms per milliliter of serum (zinc) and 2 to 15 nanograms per milliliter of serum (cadmium). In control rats given saline injections over the same period the metallothionein concentration ranged from 1 to 3 nanograms per milliliter of serum.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Garvey, J S -- Chang, C C -- ES 01629/ES/NIEHS NIH HHS/ -- New York, N.Y. -- Science. 1981 Nov 13;214(4522):805-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7292012" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cadmium/*pharmacology ; Dose-Response Relationship, Drug ; Male ; Metalloproteins/*blood ; Metallothionein/*blood/immunology ; Radioimmunoassay ; Rats ; Rats, Inbred Strains ; Zinc/*pharmacology
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    Somatomedin B: mitogenic activity derived from contaminant epidermal growth factor (1981)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1981-09-04
    Description: The mitogenic effect of somatomedin B on human cultured glial cells was neutralized by the addition of antibodies to mouse epidermal growth factor. Somatomedin B contained epidermal growth factor--like activity, competing for binding to the epidermal growth factor receptor. It is concluded that contaminating epidermal growth factor may explain the entire mitogenic activity of somatomedin B.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Heldin, C H -- Wasteson, A -- Fryklund, L -- Westermark, B -- New York, N.Y. -- Science. 1981 Sep 4;213(4512):1122-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6973821" target="_blank"〉PubMed〈/a〉
    Keywords: Cell Division/drug effects ; Cells, Cultured ; Epidermal Growth Factor/*pharmacology ; Growth Substances/*pharmacology ; Humans ; Neuroglia ; Peptides/*pharmacology ; Somatomedins/*pharmacology ; Structure-Activity Relationship
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  • 77
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    Peripherally administered reduced pterins do enter the brain (1981)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1981-05-22
    Description: The content of tetrahydrobiopterin in rat brain was doubled by peripherally administered tetrahydrobiopterin, with the natural 1 diastereoisomer more effective than the unnatural d configuration. The model pteridine, 6-methyltetrahydropterin was ten times more efficient than tetrahydrobiopterin in crossing the blood-brain barrier, and striatal concentrations of 6-methyltetrahydropterin remained elevated for 2 hours, declining with a half-life of 3 hours. While no evidence for a specific uptake mechanism for concentrating 6-methyltetrahydropterin in cells containing tetrahydrobiopterin was detected, the pterin was found in ts presumed site of action, the nerve terminal. Replacement therapy with reduced pterins may therefore be effective in the treatment of the neurological disorders associated with the variant forms of hyperphenylalaninemia that result from defects in the biosynthesis or metabolism of tetrahydrobiopterin within the central nervous system.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Kapatos, G -- Kaufman, S -- New York, N.Y. -- Science. 1981 May 22;212(4497):955-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7233193" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Biopterin/analogs & derivatives/*metabolism ; Blood-Brain Barrier ; Brain/*metabolism ; Male ; Pteridines/*metabolism ; Pterins/*metabolism ; Rats ; Stereoisomerism ; Structure-Activity Relationship
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    Odor quality: semantically generated multidimensional profiles are stable (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-11-19
    Description: Odors of ten compounds were characterized by approximately 150 subjects who used a list of 146 descriptors. Duplicate profiles correlated highly (P less than .001) and consistently higher than profiles of different odors. Profiles also agreed with those obtained previously. Thus, profiles based on combined responses of many subjects are stable constructs.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Dravnieks, A -- New York, N.Y. -- Science. 1982 Nov 19;218(4574):799-801.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7134974" target="_blank"〉PubMed〈/a〉
    Keywords: *Alcohols ; Anisoles ; Hexanols ; Humans ; *Odors ; Pyridines ; *Smell ; Structure-Activity Relationship
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    Spinal sympathetic neurons: possible sites of opiate-withdrawal suppression by clonidine (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-03-26
    Description: Morphine, methadone, meperidine, fentanyl, and clonidine rapidly depressed transmission through sympathetic preganglionic neurons in cats with the spinal cord transected. Naloxone promptly antagonized this effect of the opiates but not that of clonidine which was reversed by alpha 2-adrenergic receptor antagonists. The independent depression of preganglionic neurons by clonidine may contribute to the ability of this drug to depress the symptoms of opiate withdrawal that are characterized by sympathetic hyperactivity.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Franz, D N -- Hare, D B -- McCloskey, K L -- GM-07579/GM/NIGMS NIH HHS/ -- HL-24085/HL/NHLBI NIH HHS/ -- RR-05428/RR/NCRR NIH HHS/ -- New York, N.Y. -- Science. 1982 Mar 26;215(4540):1643-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6280276" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cats ; Clonidine/*pharmacology/therapeutic use ; Evoked Potentials/drug effects ; Humans ; Narcotics/pharmacology ; Receptors, Drug/drug effects ; Reflex/drug effects ; Spinal Cord/cytology ; Structure-Activity Relationship ; Substance Withdrawal Syndrome/*drug therapy ; Sympathetic Nervous System/*drug effects ; Synaptic Transmission/*drug effects
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  • 80
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    Circulating somatostatin acts on the islets of Langerhans by way of a somatostatin-poor compartment (1982)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1982-10-29
    Description: Somatostatin perfused in canine pancreases at 10 to 20 picograms per milliliter or 10 to 20 percent of the pancreatic vein somatostatin concentration inhibited insulin and glucagon secretion. This suggests that the high local concentration of endogenous somatostatin is not in contact with somatostatin receptors of the islets. The integrity of this separation may determine the sensitivity of islet cells to circulating somatostatin.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Kawai, K -- Ipp, E -- Orci, L -- Perrelet, A -- Unger, R H -- New York, N.Y. -- Science. 1982 Oct 29;218(4571):477-8.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6126931" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Dogs ; Dose-Response Relationship, Drug ; Glucagon/secretion ; Insulin/secretion ; Intercellular Junctions/physiology ; Islets of Langerhans/*secretion ; Receptors, Cell Surface/physiology ; Receptors, Somatostatin ; Somatostatin/*blood/metabolism
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    Homologous regulation of gonadotropin-releasing hormone receptors in cultured pituitary cells (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-02-19
    Description: Specific receptors for gonadotropin-releasing hormone (GnRH) in cultured rat pituitary cells were increased by subnanomolar concentrations of GnRH agonists and decreased by high concentrations of these peptides. The antagonist [D-Phe2, Pro3, D-Phe6]GnRH did not alter GnRH binding capacity and blocked the increase in sites induced by GnRH. These findings provide direct evidence for the homologous regulation of GnRH receptors by physiological concentrations of the hypothalamic peptide, an action that could mediate the cyclical and postcastration increases in GnRH receptors and responsiveness of the pituitary gonadotrophs.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Loumaye, E -- Catt, K J -- New York, N.Y. -- Science. 1982 Feb 19;215(4535):983-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6296998" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cells, Cultured ; Dose-Response Relationship, Drug ; Feedback ; Female ; Gonadotropin-Releasing Hormone/analogs & derivatives/metabolism/pharmacology ; Pituitary Gland/secretion ; Pituitary Hormone-Releasing Hormones/*metabolism/pharmacology ; Rats ; Receptors, Cell Surface/*pharmacology ; Receptors, LHRH
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  • 82
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    Cysteamine: a potent and specific depletor of pituitary prolactin (1982)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1982-07-30
    Description: Cysteamine rapidly reduces the concentration of prolactin in pituitary tissue in vivo and in vitro. The effect is dose-dependent, reversible, and cannot be accounted for by prolactin release. Cysteamine does not appear to exert its effect through dopamine receptors and does not alter lactotrope morphology, as determined by electron microscopy.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Millard, W J -- Sagar, S M -- Landis, D M -- Martin, J B -- AM 26252/AM/NIADDK NIH HHS/ -- New York, N.Y. -- Science. 1982 Jul 30;217(4558):452-4.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7089575" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cells, Cultured ; Cysteamine/*pharmacology ; Domperidone/pharmacology ; Dose-Response Relationship, Drug ; Kinetics ; Male ; Pituitary Gland, Anterior/*metabolism ; Prolactin/analysis/*metabolism/secretion ; Rats ; Receptors, Dopamine/physiology ; Spiperone/pharmacology
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  • 83
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    Heroin "overdose" death: contribution of drug-associated environmental cues (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-04-23
    Description: A model of "overdose" deaths among heroin addicts is proposed which emphasizes recent findings concerning the contribution of drug-associated environmental cues to drug tolerance. Results of animal experiments performed to evaluate this model suggest that conditioned drug-anticipatory responses, in addition to pharmacological factors, affect heroin-induced mortality.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Siegel, S -- Hinson, R E -- Krank, M D -- McCully, J -- New York, N.Y. -- Science. 1982 Apr 23;216(4544):436-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7200260" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Disease Models, Animal ; Dose-Response Relationship, Drug ; Drug Tolerance ; Environment ; Heroin/*pharmacology ; Humans ; Male ; Rats ; Substance-Related Disorders/*physiopathology
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  • 84
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    Diazepam impairs lateral position control in highway driving (1982)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1982-07-02
    Description: Nine expert drivers operated an instrumented vehicle in tests over a highway at night after being treated with diazepam (5 and 10 milligrams), a placebo, and nothing. They reacted to 10 milligrams of diazepam with increased lateral position variability. Potentially dangerous impairment was inferred from the reactions of some subjects.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉O'Hanlon, J F -- Haak, T W -- Blaauw, G J -- Riemersma, J B -- New York, N.Y. -- Science. 1982 Jul 2;217(4554):79-81.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7089544" target="_blank"〉PubMed〈/a〉
    Keywords: Adult ; *Automobile Driving ; Diazepam/*pharmacology ; Dose-Response Relationship, Drug ; Double-Blind Method ; Functional Laterality ; Humans ; Male ; Motor Activity/*drug effects ; Placebos
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  • 85
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    DNA conformation, dynamics, and interactions in solution (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-05-07
    Description: The conformation and dynamics of the d(CGCGAATTCGCG) duplex, its analogs containing mismatched base pairs and helix interruptions, and its complexes with actinomycin and Netropsin, bound separately and simultaneously, have been investigated by nuclear magnetic resonance spectroscopy in aqueous solution. Structural information has been deduced from chemical shift and nuclear Overhauser effect parameters, while the kinetics have been probed from line width and saturation recovery experiments on proton and phosphorus markers at the individual base pair level. These studies lead to an improved understanding of the role of nucleic acid sequence on the structure, flexibility, and conformational interconversions in the duplex state. The nuclear magnetic resonance measurements readily identify helix modification and antibiotic binding sites on the nucleic acid and estimate the extent to which the observed conformational and dynamic perturbations are transmitted to adjacent base pair regions.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Patel, D J -- Pardi, A -- Itakura, K -- New York, N.Y. -- Science. 1982 May 7;216(4546):581-90.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6280281" target="_blank"〉PubMed〈/a〉
    Keywords: Base Sequence ; Dna ; Dactinomycin ; Hydrogen Bonding ; Magnetic Resonance Spectroscopy ; Motion ; Netropsin ; *Nucleic Acid Conformation ; Oligodeoxyribonucleotides ; Protons ; Structure-Activity Relationship ; Temperature
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  • 86
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    (+)-Amphetamine binding to rat hypothalamus: relation to anorexic potency for phenylethylamines (1982)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1982-10-29
    Description: Saturable and stereospecific binding sites for (+)-[3H]amphetamine were demonstrated in membrane preparations from rat brain. The density of these binding sites varies among brain regions and is highest in the hypothalamus and brainstem. Specific (+)-[3H]amphetamine binding in hypothalamus is largely confined to synaptosomal membranes, rapidly reversible, and sensitive to both heat and proteolytic enzymes. Scatchard analysis of the equilibrium binding data revealed two distinct sites with apparent affinity constants of 93 and 300 nanomoles per liter, respectively. The effects of various psychotropic drugs as well as a number of putative neurotransmitters and related agonists and antagonists in displacing specific (+)-[3H]amphetamine binding demonstrate that these binding sites are not associated with any previously described neurotransmitter or drug receptors, but are specific for amphetamine and related phenylethylamine derivatives. Furthermore, the relative affinities of a series of phenylethylamine derivatives for (+)-[3H]amphetamine binding sites in hypothalamic membranes is highly correlated to their potencies as anorexic agents. These results suggest the presence of specific receptor sites in hypothalamus that mediate the anorexic activity of amphetamine and related drugs.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Paul, S M -- Hulihan-Giblin, B -- Skolnick, P -- New York, N.Y. -- Science. 1982 Oct 29;218(4571):487-90.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7123250" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Anorexia/physiopathology ; Appetite Depressants/*pharmacology ; Cell Membrane/metabolism ; Dextroamphetamine/*metabolism ; Hypothalamus/drug effects/*metabolism/physiology ; Male ; Phenethylamines/metabolism ; Rats ; Receptors, Drug/*metabolism ; Structure-Activity Relationship
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  • 87
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    Nonopiate effects of dynorphin and des-Tyr-dynorphin (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-12-10
    Description: Intracerebroventricular administration of dynorphin produced potent and long-lasting effects on motor function and the electroencephalogram in rats. In addition, local iontophoretic or pressure ejection of dynorphin consistently inhibited hippocampal unit activity. None of these effects were significantly affected by naloxone even at high doses. Moreover, a fragment of dynorphin that failed to displace any of a number of tritiated narcotics from rat brain homogenates produced similar effects on these physiological measures in vivo. On the basis of a variety of criteria for "opiate action," the results suggest that a second biologically active site within the dynorphin sequence is capable of quite potent but nonopiate effects.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Walker, J M -- Moises, H C -- Coy, D H -- Baldrighi, G -- Akil, H -- 1F32DA04183/DA/NIDA NIH HHS/ -- DA02265/DA/NIDA NIH HHS/ -- New York, N.Y. -- Science. 1982 Dec 10;218(4577):1136-8.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6128791" target="_blank"〉PubMed〈/a〉
    Keywords: Action Potentials ; Amino Acid Sequence ; Animals ; Dynorphins ; Endorphins/*physiology ; Hippocampus/*physiology ; Male ; Pain/*physiopathology ; Rats ; Structure-Activity Relationship
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  • 88
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    Glucose stimulation of the antilipolytic effect of insulin in humans (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-06-03
    Description: Dose-response studies of the inhibition of lipolysis by insulin in isolated human adipocytes were conducted with the use of a sensitive bioluminescent assay of glycerol release. The addition of glucose to the incubation medium was associated with an increase in insulin sensitivity and an increase in the maximum insulin effect. The results suggest that glucose plays an important role in regulating the antilipolytic action of insulin in humans.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Arner, P -- Bolinder, J -- Ostman, J -- New York, N.Y. -- Science. 1983 Jun 3;220(4601):1057-9.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6342138" target="_blank"〉PubMed〈/a〉
    Keywords: Adipose Tissue/cytology ; Cells, Cultured ; Dose-Response Relationship, Drug ; Drug Synergism ; Glucose/*pharmacology ; Humans ; Insulin/*pharmacology ; Isoproterenol/pharmacology ; Lipolysis/*drug effects
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  • 89
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    Bronchoconstrictor effects of leukotriene C in humans (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-04-09
    Description: Maximum expiratory flow rate at 30 percent of vital capacity above residual volume served as an index of airway obstruction in comparing the effects of leukotriene C and histamine administered by aerosol to five normal persons. Leukotriene C was 600 to 9500 times more potent than histamine on a molar basis in producing an equivalent decrement in the residual volume. The leukotriene C response was slow in onset and prolonged, reminiscent of the effects of aerosol allergen challenge in asthmatic allergic subjects.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Weiss, J W -- Drazen, J M -- Coles, N -- McFadden, E R Jr -- Weller, P F -- Corey, E J -- Lewis, R A -- Austen, K F -- AI-00399/AI/NIAID NIH HHS/ -- AI-07722/AI/NIAID NIH HHS/ -- AI-10356/AI/NIAID NIH HHS/ -- New York, N.Y. -- Science. 1982 Apr 9;216(4542):196-8.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7063880" target="_blank"〉PubMed〈/a〉
    Keywords: Adult ; Airway Resistance/*drug effects ; Bronchi/*drug effects ; Dose-Response Relationship, Drug ; Female ; Histamine/pharmacology ; Humans ; Male ; Middle Aged ; Prostaglandins F/pharmacology ; SRS-A/*pharmacology ; Time Factors
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  • 90
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    A major metabolite of arginine vasopressin in the brain is a highly potent neuropeptide (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-09-23
    Description: A peptide that accumulated as the major product during the proteolysis of arginine vasopressin by rat brain synaptic membranes was isolated and its structure was shown to be the hexapeptide pGlu-Asn-Cys(Cys)-Pro-Arg-Gly-NH2. When administered intracerebroventricularly in extremely low doses, this vasopressin fragment and its desglycinamide derivative facilitated memory consolidation in a passive avoidance situation. These vasopressin metabolites, which are devoid of pressor activity, constitute highly potent neuropeptides with selective effects on memory and related processes; they are activated via proteolytic processing of vasopressin by brain peptidases.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Burbach, J P -- Kovacs, G L -- de Wied, D -- van Nispen, J W -- Greven, H M -- New York, N.Y. -- Science. 1983 Sep 23;221(4617):1310-2.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6351252" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Animals ; Arginine Vasopressin/*metabolism/physiology ; Avoidance Learning/physiology ; Brain/*metabolism ; Dose-Response Relationship, Drug ; Male ; Memory/*physiology ; Oligopeptides/metabolism ; Peptide Hydrolases/metabolism ; Rats ; Structure-Activity Relationship
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  • 91
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    Ethanol modulation of opiate receptors in cultured neural cells (1983)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1983-12-16
    Description: The mouse neuroblastoma-rat glioma hybrid cell line NG108-15 was used to study the acute and chronic interaction of ethanol with intact neural cells. In the short term, ethanol inhibited opiate receptor binding, but after long-term exposure the cells exhibited an apparent adaptive increase in the number of opiate binding sites; this was reversible when ethanol was withdrawn. High concentrations of ethanol (200 mM) increased opiate binding after 18 to 24 hours, whereas lower concentrations (25 to 50 mM) produced similar changes after 2 weeks. This model system has potential for exploring the cellular and molecular mechanisms underlying ethanol intoxication, tolerance, and withdrawal.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Charness, M E -- Gordon, A S -- Diamond, I -- New York, N.Y. -- Science. 1983 Dec 16;222(4629):1246-8.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6316506" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cell Line ; Dose-Response Relationship, Drug ; Enkephalin, Methionine/analogs & derivatives/metabolism ; Ethanol/*pharmacology ; Glioma ; Hybrid Cells ; Mice ; Neuroblastoma ; Neurons/*drug effects/metabolism ; Rats ; Receptors, Opioid/*drug effects/metabolism ; Time Factors
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  • 92
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    Fluoride directly stimulates proliferation and alkaline phosphatase activity of bone-forming cells (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-10-21
    Description: Fluoride is one of the most potent but least well understood stimulators of bone formation in vivo. Bone formation was shown to arise from direct effects on bone cells. Treatment with sodium fluoride increased proliferation and alkaline phosphatase activity of bone cells in vitro and increased bone formation in embryonic calvaria at concentrations that stimulate bone formation in vivo.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Farley, J R -- Wergedal, J E -- Baylink, D J -- AM31061/AM/NIADDK NIH HHS/ -- AM31062/AM/NIADDK NIH HHS/ -- New York, N.Y. -- Science. 1983 Oct 21;222(4621):330-2.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6623079" target="_blank"〉PubMed〈/a〉
    Keywords: Alkaline Phosphatase/*metabolism ; Animals ; Bone Development/*drug effects ; Bone and Bones/*cytology/embryology/enzymology ; Cell Division/drug effects ; Cells, Cultured ; Chick Embryo ; Dose-Response Relationship, Drug ; Fluorides/*pharmacology ; Parathyroid Hormone/pharmacology
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  • 93
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    A functional role for an opiate system in snail thermal behavior (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-04-01
    Description: The terrestrial snail Cepaea nemoralis, when placed on a 40 degrees C hot plate, lifts the anterior portion of its foot. The latency of this response is influenced by morphine and by naloxone in a dose-dependent and time-dependent manner. Morphine increases the time taken to respond, whereas naloxone reduces it. Furthermore, naloxone abolishes the effect of morphine. These results indicate that an opiate system may have a role in this behavior, which resembles that reported in vertebrates.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Kavaliers, M -- Hirst, M -- Teskey, G C -- New York, N.Y. -- Science. 1983 Apr 1;220(4592):99-101.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6298941" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Behavior, Animal/drug effects/*physiology ; Dose-Response Relationship, Drug ; Hot Temperature ; Morphine/pharmacology ; Naloxone/pharmacology ; Receptors, Opioid/drug effects/*physiology ; Snails/*physiology ; Thermoreceptors/physiology
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  • 94
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    Substance P and somatostatin regulate sympathetic noradrenergic function (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-09-09
    Description: Peptidergic-noradrenergic interactions were examined in explants of rat sympathetic superior cervical ganglia and in cultures of dissociated cells. The putative peptide transmitters substance P and somatostatin each increased the activity of the catecholamine-synthesizing enzyme tyrosine hydroxylase after 1 week of exposure in culture. Maximal increases occurred at 10(-7) molar for each peptide, and either increasing or decreasing the concentration reduced the effects. Similar increases in tyrosine hydroxylase were produced by a metabolically stable agonist of substance P, while a substance P antagonist prevented the effects of the agonist. The data suggest that the increased tyrosine hydroxylase activity was mediated by peptide interaction with specific substance P receptors and that peptides may modulate sympathetic catecholaminergic function.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Kessler, J A -- Adler, J E -- Black, I B -- New York, N.Y. -- Science. 1983 Sep 9;221(4615):1059-61.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6192502" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Bacitracin/pharmacology ; Captopril/pharmacology ; Cells, Cultured ; Culture Techniques ; Dose-Response Relationship, Drug ; Ganglia, Sympathetic/*enzymology ; Rats ; Somatostatin/*pharmacology ; Substance P/*pharmacology ; Tyrosine 3-Monooxygenase/*metabolism
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  • 95
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    Pregnancy increases reactivity of mice to phenobarbital (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-04-29
    Description: Compared to nonpregnant controls, pregnant mice injected with phenobarbital had lower concentrations of the drug in the plasma but equivalent concentrations in the brain. In spite of the similar concentrations in the brain, the behavioral response to phenobarbital was greater for pregnant than nonpregnant mice. These results suggest that the concentration of phenobarbital in the plasma, which is commonly used as a basis for adjusting phenobarbital dosage during pregnancy, is not an appropriate indicator of the dynamics of the drug.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Middaugh, L D -- Zemp, J W -- Boggan, W O -- AA03532/AA/NIAAA NIH HHS/ -- DA00041/DA/NIDA NIH HHS/ -- DA01750/DA/NIDA NIH HHS/ -- New York, N.Y. -- Science. 1983 Apr 29;220(4596):534-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6836299" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Brain Chemistry ; Dose-Response Relationship, Drug ; Female ; Humans ; Mice ; Mice, Inbred C57BL ; Motor Activity/drug effects ; Phenobarbital/analysis/*metabolism/pharmacology ; *Pregnancy/drug effects ; Time Factors
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  • 96
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    Antipyretic potency of centrally administered alpha-melanocyte stimulating hormone (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-07-08
    Description: Centrally administered alpha-melanocyte stimulating hormone is much more potent in reducing fever than the widely used antipyretic acetaminophen. This finding supports the hypothesis that the endogenous neuropeptide has a role in the limitation of fever and suggests that it may be clinically useful as an antipyretic.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Murphy, M T -- Richards, D B -- Lipton, J M -- NS 10046/NS/NINDS NIH HHS/ -- New York, N.Y. -- Science. 1983 Jul 8;221(4606):192-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6602381" target="_blank"〉PubMed〈/a〉
    Keywords: Acetaminophen/pharmacology ; Animals ; Anti-Inflammatory Agents, Non-Steroidal/*pharmacology ; Body Temperature/drug effects ; Dose-Response Relationship, Drug ; Fever/drug therapy ; Humans ; Melanocyte-Stimulating Hormones/*pharmacology ; Rabbits
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  • 97
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    Somatomedin-C mediates growth hormone negative feedback by effects on both the hypothalamus and the pituitary (1981)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1981-06-12
    Description: Somatomedin-C stimulates somatostatin release to a maximum of 390 percent of basal release during short-term (20-minute) incubation of rat hypothalamus. It has no effect on basal or stimulated growth hormone release from primary cultures of rat adenohypophyseal cells during a 4-hour incubation, but inhibits stimulated release by more that 90 percent after 24 hours. These findings suggest that somatomedin-C participates in the growth hormone negative feedback loop with an immediate effect on hypothalamic somatostatin and a delayed effect on the anterior pituitary.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Berelowitz, M -- Szabo, M -- Frohman, L A -- Firestone, S -- Chu, L -- Hintz, R L -- AM 18722/AM/NIADDK NIH HHS/ -- AM 24085/AM/NIADDK NIH HHS/ -- New York, N.Y. -- Science. 1981 Jun 12;212(4500):1279-81.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6262917" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Bucladesine/pharmacology ; Cells, Cultured ; Dose-Response Relationship, Drug ; Feedback ; Growth Hormone/pharmacology/*secretion ; Hypothalamus/drug effects/*physiology ; Insulin-Like Growth Factor I ; Kinetics ; Pituitary Gland, Anterior/drug effects/*secretion ; Rats ; Somatomedins/*pharmacology
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  • 98
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    Interaction between purine and benzodiazepine: Inosine reverses diazepam-induced stimulation of mouse exploratory behavior (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-02-13
    Description: Inosine, 2-deoxyinosine, and 2-deoxyguanosine completely reversed the increase in exploratory activity elicited in mice by diazepam. The inhibition of exploratory behavior by purines occurred at doses that when given alone have no effect on exploratory behavior. 7-Methylinosine, which does not bind to the brain benzodiazepine binding site in vitro, had no effect on the diazepam-induced increase in exploratory behavior. Behavioral effects produced by various combinations of inosine and diazepam indicate that the interaction between purine and benzodiazepine is antagonistic and support the hypothesis that the naturally occurring purines function in anxiety-related behaviors that respond to benzodiazepine treatment.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Crawley, J N -- Marangos, P J -- Paul, S M -- Skolnick, P -- Goodwin, F K -- New York, N.Y. -- Science. 1981 Feb 13;211(4483):725-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6256859" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Anxiety/*drug effects ; Behavior, Animal/drug effects ; Diazepam/*antagonists & inhibitors ; Dose-Response Relationship, Drug ; Humans ; Inosine/*pharmacology ; Male ; Mice ; Receptors, Drug/*drug effects ; Receptors, GABA-A
    Print ISSN: 0036-8075
    Electronic ISSN: 1095-9203
    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
    Published by American Association for the Advancement of Science (AAAS)
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  • 99
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    Heart imaging with cationic complexes of technetium (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-10-02
    Description: The cationic technetium-99 complex trans-[99TC(dmpe)2Cl2]+, where dmpe is bis(1,2-dimethylphosphino)ethane or (CH3)2P-CH2-P(CH3)2, has been prepared and characterized by single-crystal, x-ray structural analysis. The technetium-99m analog, trans-(99mTc(dmpe) 2Cl2]+, has also been prepared and shown to yield excellent gamma-ray images of the heart. The purposeful design, characterization, and synthesis of this technetium-99m radiopharmaceutical represents a striking application of fundamental inorganic chemistry to a problem in applied nuclear medicine.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Deutsch, E -- Bushong, W -- Glavan, K A -- Elder, R C -- Sodd, V J -- Scholz, K L -- Fortman, D L -- Lukes, S J -- HL-21276/HL/NHLBI NIH HHS/ -- New York, N.Y. -- Science. 1981 Oct 2;214(4516):85-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6897930" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cations, Monovalent ; Dogs ; Heart/*radionuclide imaging ; *Organotechnetium Compounds ; *Phosphines ; Structure-Activity Relationship ; *Technetium
    Print ISSN: 0036-8075
    Electronic ISSN: 1095-9203
    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
    Published by American Association for the Advancement of Science (AAAS)
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    Response artifact in the measurement of neuroleptic-induced anhedonia (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-07-17
    Description: Systemic administration of the neuroleptic drug alpha-flupenthixol attenuated lever-pressing behavior in rats responding for rewarding brain stimulation. The magnitude of this attenuation was dose-dependent and resembled the effects of reward reduction and termination. However, when the operant response requirements of the same rats were changed to nose poking, identical drug treatments produced relatively little attenuation in performance. These data do not support the belief that neuroleptics produce a general state of anhedonia. Rather, the apparent suppression of reinforced behaviors depends at least in part on the kinetic requirements of the response.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Ettenberg, A -- Koob, G F -- Bloom, F E -- New York, N.Y. -- Science. 1981 Jul 17;213(4505):357-9.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7244622" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Brain/physiology ; Conditioning (Psychology)/*drug effects ; Dose-Response Relationship, Drug ; Electroshock ; Flupenthixol/*pharmacology ; Male ; Rats ; *Reward ; Thioxanthenes/*pharmacology
    Print ISSN: 0036-8075
    Electronic ISSN: 1095-9203
    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
    Published by American Association for the Advancement of Science (AAAS)
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