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  • Dose-Response Relationship, Drug  (64)
  • Structure-Activity Relationship  (58)
  • American Association for the Advancement of Science (AAAS)  (115)
  • American Association for the Advancement of Science
  • Nature Publishing Group
  • 1980-1984  (115)
  • 1925-1929
  • 1983  (38)
  • 1981  (36)
  • 1980  (41)
Collection
Keywords
Publisher
  • American Association for the Advancement of Science (AAAS)  (115)
  • American Association for the Advancement of Science
  • Nature Publishing Group
Years
  • 1980-1984  (115)
  • 1925-1929
Year
  • 1983  (38)
  • 1981  (36)
  • 1980  (41)
  • 1984  (22)
  • 1982  (30)
  • 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
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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
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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
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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
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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
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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
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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
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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
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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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    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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    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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  • 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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    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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  • 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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    2,4,5-trichlorophenoxyacetic acid causes behavioral effects in chickens at environmentally relevant doses (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    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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    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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    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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    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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    Alcohol and pregnancy (1983)
    American Association for the Advancement of Science (AAAS)
    Details
    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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  • 29
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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)
    Details
    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)
    Details
    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)
    Details
    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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  • 37
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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)
    Details
    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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  • 41
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    Carbocyclic arabinofuranosyladenine (cyclaradine): efficacy against genital herpes in guinea pigs (1983)
    American Association for the Advancement of Science (AAAS)
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    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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    Nicarbazin complex yields dinitrocarbanilide as ultrafine crystals with improved anticoccidial activity (1983)
    American Association for the Advancement of Science (AAAS)
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    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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    Bromine residue at hydrophilic region influences biological activity of aplysiatoxin, a tumor promoter (1983)
    American Association for the Advancement of Science (AAAS)
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    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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    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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    Interchangeability of stress and amphetamine in sensitization (1980)
    American Association for the Advancement of Science (AAAS)
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    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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    Excitatory and inhibitory effects of serotonin on sensorimotor reactivity measured with acoustic startle (1980)
    American Association for the Advancement of Science (AAAS)
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    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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    Endorphin-mediated increases in pain threshold during pregnancy (1980)
    American Association for the Advancement of Science (AAAS)
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    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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  • 48
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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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    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)
    Details
    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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  • 52
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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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  • 53
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    Peripherally administered reduced pterins do enter the brain (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    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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  • 54
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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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    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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    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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    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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    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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    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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    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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  • 61
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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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  • 62
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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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  • 63
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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)
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    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
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    Heart imaging with cationic complexes of technetium (1981)
    American Association for the Advancement of Science (AAAS)
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    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
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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
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    Carcinogens and regulation (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-01-23
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Lappe, M -- Hooper, K -- Blake, E -- Pfund, N -- Gardner, E -- Rosenberg, J -- New York, N.Y. -- Science. 1981 Jan 23;211(4480):332-4.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7221543" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Biological Assay ; *Carcinogens ; Dose-Response Relationship, Drug ; Humans ; Species Specificity
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    Elastin fragments attract macrophage precursors to diseased sites in pulmonary emphysema (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-05-22
    Description: This study suggests one mechanism by which alveolar macrophages accumulate in the lung in pulmonary emphysema: elastin fragments generated at the diseased sites are potent chemoattractants for monocytes, the precursors of the macrophages. The most chemotactic elastin fragments have a molecular weight between 10,000 and 50,000 and are active at concentrations as low as 3 nanograms per milliliter. By comparison, elastin fragments with higher molecular weights and desmosines are active at concentrations greater than 0.3 microgram per milliliter. In addition, preincubation of monocytes with the 10,000- to 50,000-dalton elastin impairs the ability of the cells to migrate toward elastin fragments but not toward activated serum. Fragments of tropoelastin are not chemotactic for monocytes. Because elastin, but not tropoelastin, contains lysyl-derived cross-links, these structures may be the active chemotactic site on the elastin fragments.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Hunninghake, G W -- Davidson, J M -- Rennard, S -- Szapiel, S -- Gadek, J E -- Crystal, R G -- New York, N.Y. -- Science. 1981 May 22;212(4497):925-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7233186" target="_blank"〉PubMed〈/a〉
    Keywords: Cells, Cultured ; Chemotaxis, Leukocyte/*drug effects ; Dose-Response Relationship, Drug ; Elastin/*analogs & derivatives/*pharmacology ; Humans ; Macrophages/physiology ; Monocytes/*physiology ; Peptide Fragments/pharmacology ; Pulmonary Emphysema/*physiopathology ; Structure-Activity Relationship ; Tropoelastin/*pharmacology
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    A new generation of antibiotics (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-09-11
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Maugh, T H 2nd -- New York, N.Y. -- Science. 1981 Sep 11;213(4513):1238.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7268430" target="_blank"〉PubMed〈/a〉
    Keywords: Anti-Bacterial Agents/*isolation & purification ; Lactams/*isolation & purification ; Structure-Activity Relationship
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    Prudent practices for handling hazardous chemicals in laboratories (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-02-20
    Description: A National Research Council report has recommended practices for safe handling and disposal of hazardous chemicals in laboratories. They are a practical alternative to detailed regulations on individual chemicals.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉McKusick, B C -- New York, N.Y. -- Science. 1981 Feb 20;211(4484):777-80.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7466359" target="_blank"〉PubMed〈/a〉
    Keywords: Air Pollutants, Occupational/adverse effects ; Dose-Response Relationship, Drug ; Explosions/prevention & control ; Laboratories/*standards ; *Occupational Medicine ; Research ; Ventilation
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    Pineal N-acetyltransferase is inactivated by disulfide-containing peptides: insulin is the most potent (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-07-31
    Description: Pineal N-acetyltransferase can be inactivated in broken cell preparations by cystamine through a mechanism of thiol-disulfide exchange. Some, but not all, disulfide-containing peptides can inactivate this enzyme; the most potent inactivator is insulin. These findings suggest that a disulfide-containing peptide with high reactivity toward N-acetyltransferase may participate in the intracellular regulation of this enzyme.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Namboodiri, M A -- Favilla, J T -- Klein, D C -- New York, N.Y. -- Science. 1981 Jul 31;213(4507):571-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7017937" target="_blank"〉PubMed〈/a〉
    Keywords: Acetyltransferases/*antagonists & inhibitors ; Animals ; Disulfides/pharmacology ; Dithiothreitol/pharmacology ; Hormones/pharmacology ; Hydrogen-Ion Concentration ; Insulin/*pharmacology ; Kinetics ; Male ; Peptides/*pharmacology ; Pineal Gland/*enzymology ; Rats ; Structure-Activity Relationship
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    Ranking animal carcinogens: a proposed regulatory approach (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-11-20
    Description: The nature and extent of positive evidence associated with animal carcinogens vary widely, yet present regulatory policy does not permit adequate discrimination among the many carcinogenic substances. Most are treated as if they pose equal potential risk to humans, and this is not consistent with the available data. Without knowledge of carcinogenic mechanisms, the evaluation of responses in intact mammalian surrogates best reflects the potential levels of human risk. An example of a scoring system is proposed by which animal carcinogens are ranked according to the most relevant toxicological evidence derived from animal and genotoxicity studies. Different classes of animal carcinogens could thus be recognized and would permit several regulatory options and provide a means to establish priorities for public and scientific concerns.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Squire, R A -- New York, N.Y. -- Science. 1981 Nov 20;214(4523):877-80.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7302565" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; *Carcinogens/toxicity ; Dose-Response Relationship, Drug ; Drug Evaluation, Preclinical/*methods ; Humans ; Neoplasms/chemically induced ; Neoplasms, Experimental/*chemically induced ; Risk
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    Thyrotropin-releasing hormone effects in the central nervous system: dependence on arousal state (1981)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1981-11-06
    Description: Thyrotropin-releasing hormone was microinjected into the dorsal hippocampus of ground squirrels (Citellus lateralis) when they were at different levels of arousal, as assessed by electrophysiological and behavioral criteria. When administered to the awake animal, thyrotropin-releasing hormone produced dose-dependent decreases in body temperature accompanied by behavioral quieting and reductions in metabolic rate and electromyographic activity. The magnitude of these effects was greater when the peptide was microinjected during a period of behavioral activation. In contrast, administration of the peptide during slow wave sleep produced increased thermogenesis, an increase in electromyographic activity, and an increase in the amount of electroencephalographic desynchronization.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Stanton, T L -- Bechman, A L -- Winokur, A -- New York, N.Y. -- Science. 1981 Nov 6;214(4521):678-81.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6794147" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Arousal/*drug effects ; Body Temperature Regulation/*drug effects ; Dose-Response Relationship, Drug ; Female ; Hippocampus/*drug effects ; Male ; Sciuridae/*physiology ; Thyrotropin-Releasing Hormone/*pharmacology ; Wakefulness/drug effects
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    Cerebroventricular propranolol elevates cerebrospinal fluid norepinephrine and lowers blood pressure (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-08-21
    Description: Ventriculocisternal administration of dl- and d-propranolol produced dose-dependent increases in cerebrospinal fluid norepinephrine and reductions in blood pressure. A highly significant correlation was found between the increase in norepinephrine and the hypotensive effect. The propranolol-induced hypotension was prevented by intracisternal phentolamine. These data indicate that the hypotensive effect of centrally administered propranolol results from a drug-induced release of norepinephrine, which stimulates central alpha receptors to lower arterial pressure.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Tackett, R L -- Webb, J G -- Privitera, P J -- 5T32 HL07260-02/HL/NHLBI NIH HHS/ -- GM 20387/GM/NIGMS NIH HHS/ -- New York, N.Y. -- Science. 1981 Aug 21;213(4510):911-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7256285" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Blood Pressure/*drug effects ; Dogs ; Injections, Intraventricular ; Isomerism ; Norepinephrine/*cerebrospinal fluid ; Propranolol/administration & dosage/*pharmacology ; Structure-Activity Relationship
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    Characterization of a 41-residue ovine hypothalamic peptide that stimulates secretion of corticotropin and beta-endorphin (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-09-18
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Vale, W -- Spiess, J -- Rivier, C -- Rivier, J -- AM 18811/AM/NIADDK NIH HHS/ -- AM 20917/AM/NIADDK NIH HHS/ -- AM 26741/AM/NIADDK NIH HHS/ -- New York, N.Y. -- Science. 1981 Sep 18;213(4514):1394-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6267699" target="_blank"〉PubMed〈/a〉
    Keywords: Adrenocorticotropic Hormone/*secretion ; Amino Acid Sequence ; Amphibian Proteins ; Angiotensinogen ; Animals ; Corticotropin-Releasing Hormone/*isolation & purification ; Endorphins/*secretion ; Hypothalamo-Hypophyseal System/physiology ; Peptide Hormones ; Peptides ; Pituitary Gland, Anterior/*secretion ; Pituitary Hormone-Releasing Hormones/*isolation & purification ; Radioimmunoassay ; Sheep ; Structure-Activity Relationship
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    Ivermectin: a potent new antiparasitic agent (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-08-26
    Description: Ivermectin is the 22,23-dihydro derivative of avermectin B1, a macrocyclic lactone produced by an actinomycete, Streptomyces avermitilis. It is active at extremely low dosage against a wide variety of nematode and arthropod parasites, apparently by virtue of its action on the mediation of neurotransmission by gamma-aminobutyric acid. It is now in commercial use in various countries for the treatment and control of parasites in cattle, horses, and sheep, and is expected to become available for use in swine and dogs. Since studies with the drug in man are in a preliminary stage, it is not yet known whether ivermectin will be useful in human medicine.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Campbell, W C -- Fisher, M H -- Stapley, E O -- Albers-Schonberg, G -- Jacob, T A -- New York, N.Y. -- Science. 1983 Aug 26;221(4613):823-8.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6308762" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; *Anthelmintics ; Arthropods/drug effects ; Humans ; Insecticides/therapeutic use ; Ivermectin ; Lactones/metabolism/pharmacology/*therapeutic use ; Nematode Infections/*drug therapy ; Streptomyces/physiology ; Structure-Activity Relationship ; Synaptic Transmission/drug effects
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    Stereospecific action of pyrethroid insecticides on the gamma-aminobutyric acid receptor-ionophore complex (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-09-30
    Description: The potent alpha-cyano-3-phenoxybenzyl pyrethroids, including cypermethrin, deltamethrin, and fenvalerate, act stereospecifically to inhibit binding to rat brain synaptic membranes of sulfur-35-labeled t-butylbicyclophosphorothionate, a new radioligand for the picrotoxinin binding site. Scatchard analysis indicates that picrotoxinin inhibition of t-butylbicyclophosphorothionate binding is competitive whereas cypermethrin inhibition possibly involves a closely associated site in the gamma-aminobutyric acid receptor-ionophore complex. Studies with 37 pyrethroids reveal an absolute correlation, that is, no false positives or negatives, between mouse intracerebral toxicity and in vitro inhibition: all toxic cyano compounds but none of their nontoxic stereoisomers are inhibitors; cis isomers are more potent than trans isomers as both toxicants and inhibitors; and noncyano pyrethroids are much less potent or are inactive.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Lawrence, L J -- Casida, J E -- P01 ES00049/ES/NIEHS NIH HHS/ -- New York, N.Y. -- Science. 1983 Sep 30;221(4618):1399-401.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6310756" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Bicyclo Compounds/metabolism ; *Bicyclo Compounds, Heterocyclic ; Binding, Competitive ; Brain/metabolism ; Insecticides/*pharmacology ; Ionophores/antagonists & inhibitors ; Picrotoxin/metabolism ; Protein Binding ; Pyrethrins/metabolism/*pharmacology ; Rats ; Receptors, Cell Surface/*drug effects/metabolism ; Receptors, GABA-A ; Stereoisomerism ; Structure-Activity Relationship ; Synaptic Membranes/metabolism
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    5-hydroxytryptophan elevates serum melatonin (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-08-12
    Description: Daytime administration of 5-hydroxytryptophan to sheep elevated serum melatonin more than sevenfold within 2 hours. This suggests that administration of 5-hydroxytryptophan could be used as the basis of a clinical test of pineal function and that melatonin might mediate some clinical effects of 5-hydroxytryptophan.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Namboodiri, M A -- Sugden, D -- Klein, D C -- Mefford, I N -- New York, N.Y. -- Science. 1983 Aug 12;221(4611):659-61.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6867734" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Dose-Response Relationship, Drug ; Humans ; Male ; Melatonin/*blood ; Pineal Gland/physiology ; Rats ; Serotonin/*pharmacology ; Sheep ; Tryptophan/pharmacology
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    Spermidine requirement for cell proliferation in eukaryotic cells: structural specificity and quantitation (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-03-04
    Description: Six structural homologs of spermidine and five of its precursor, putrescine, were studied for their ability to prevent cytostasis of cultured L1210 leukemia cells induced by alpha-difluoromethylornithine (DFMO), a specific inhibitor of putrescine biosynthesis. High-performance liquid chromatography and competition studies with spermidine indicated that the homologs, which vary in the length of the carbon chain separating the amines, penetrated the cells. The structural specificity of the spermidine carrier was defined. Three of the six spermidine homologs supported cell growth during a 48-hour incubation in the presence of DFMO, indicating that a two-carbon extension of spermidine structure was tolerated for biological function. Two of the five putrescine homologs supported growth after being converted by the cells to their respective spermidine homologs. The central nitrogen of spermidine appears to be essential for function since diamines of chain length comparable to that of spermidine did not prevent DFMO cytostasis. No more than 15 percent of the spermidine normally present in L1210 cells was required for cell proliferation in the presence of DFMO.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Porter, C W -- Bergeron, R J -- CA-22153/CA/NCI NIH HHS/ -- CA-24538/CA/NCI NIH HHS/ -- New York, N.Y. -- Science. 1983 Mar 4;219(4588):1083-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6823570" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; *Cell Division ; *Cell Physiological Phenomena ; Eukaryotic Cells/*physiology ; Leukemia L1210/pathology ; Mice ; Ornithine Decarboxylase Inhibitors ; Putrescine/physiology ; Spermidine/analogs & derivatives/*physiology ; Structure-Activity Relationship
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    Hysteresis in the force-calcium relation in muscle (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-03-04
    Description: Calcium ions activate muscle contraction. The mechanism depends on the calcium sensitivity of the proteins that regulate contraction. Evidence is presented for the reverse phenomenon, where contraction modulates calcium sensitivity. Increasing the force level increased calcium sensitivity in intact fibers showing that the relation between force and calcium is not unique. A particular calcium concentration can maintain a higher force level than it can create. The results were confirmed in skinned fiber experiments. Transient reduction of the force led to a transient reduction in calcium binding, suggesting a simple mechanism for the hysteresis.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Ridgway, E B -- Gordon, A M -- Martyn, D A -- NS 08384/NS/NINDS NIH HHS/ -- NS 10919/NS/NINDS NIH HHS/ -- New York, N.Y. -- Science. 1983 Mar 4;219(4588):1075-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6823567" target="_blank"〉PubMed〈/a〉
    Keywords: Aequorin ; Animals ; Calcium/metabolism/*physiology ; Dose-Response Relationship, Drug ; *Muscle Contraction ; Protein Binding ; Thoracica
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    Is thymosin action mediated by prostaglandin release? (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-06-10
    Description: Treatment of spleen cells derived from adult thymectomized mice with thymosin fraction 5 resulted in a rapid and dose-dependent stimulation of the release of immunoreactive prostaglandin E2. The release of prostaglandin E2 was associated with induction of theta antigen and was totally inhibited by indomethacin. In contrast, prostaglandin E2 release from spleen cells from intact donors was inhibited by treatment with fraction 5. The data support the concept that prostaglandin E2 mediates the effects of thymosin fraction 5 on lymphocytes.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Rinaldi Garaci, C -- Favalli, C -- Del Gobbo, V -- Garaci, E -- Jaffe, B M -- New York, N.Y. -- Science. 1983 Jun 10;220(4602):1163-4.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6574601" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Dinoprostone ; Dose-Response Relationship, Drug ; Indomethacin/pharmacology ; Lymphocytes/drug effects/physiology ; Male ; Mice ; Mice, Inbred C57BL ; Prostaglandins E/*physiology ; Spleen/drug effects/physiology ; Thymectomy ; Thymosin/*pharmacology ; Thymus Hormones/*pharmacology
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    Bodian's silver method stains neurofilament polypeptides (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-09-25
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Gambetti, P -- Autilio Gambetti, L -- Papasozomenos, S C -- AG 00795/AG/NIA NIH HHS/ -- NS 14509/NS/NINDS NIH HHS/ -- New York, N.Y. -- Science. 1981 Sep 25;213(4515):1521-2.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6169146" target="_blank"〉PubMed〈/a〉
    Keywords: Cytoskeleton/*ultrastructure ; Electrophoresis, Polyacrylamide Gel ; Molecular Weight ; Proteins ; Silver ; *Staining and Labeling ; Structure-Activity Relationship
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    Side-effect reduction by use of drugs that bind to separate but equivalent binding sites (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-12-18
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Ehrenstein, G -- Huang, L Y -- New York, N.Y. -- Science. 1981 Dec 18;214(4527):1365-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7313696" target="_blank"〉PubMed〈/a〉
    Keywords: Binding Sites ; Dose-Response Relationship, Drug ; Drug Synergism ; *Drug-Related Side Effects and Adverse Reactions ; Models, Biological ; Receptors, Drug/*drug effects
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    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 83
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    Metkephamid, a systemically active analog of methionine enkephalin with potent opioid alpha-receptor activity (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-02-06
    Description: Metkephamid is an analog of methionine enkephalin that retains high affinity for the delta receptor and is a systemically active analgesic. Since it is at least 100 times more potent than morphine as an analgesic when placed directly into the lateral ventricles, and is 30 to 100 times more potent on the delta receptor and yet is roughly equipotent on the mu receptor in vitro, it is concluded that it probably produces analgesia by action on delta receptors as well as, or rather than, on mu receptors. It has less tendency to produce respiratory depression, tolerance, and physical dependence than standard analgesics, and it is presently undergoing clinical trial.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Frederickson, R C -- Smithwick, E L -- Shuman, R -- Bemis, K G -- New York, N.Y. -- Science. 1981 Feb 6;211(4482):603-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6256856" target="_blank"〉PubMed〈/a〉
    Keywords: *Analgesics ; Animals ; Brain/*drug effects ; Dose-Response Relationship, Drug ; Endorphins/*pharmacology ; *Enkephalin, Methionine/*analogs & derivatives ; Enkephalins/*pharmacology ; Humans ; Kinetics ; Male ; Mice ; Rats ; Receptors, Opioid/*drug effects ; Structure-Activity Relationship ; Substance-Related Disorders/etiology
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    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 84
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    A substance P antagonist, [D-Pro2, D-Trp7,9]SP, inhibits inflammatory responses in the rabbit eye (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-11-27
    Description: Neurogenic factors released by antidromic nerve stimulation are thought to be in part responsible for the vasodilation and breakdown of the blood-aqueous barrier that follows trauma to the eye. Substance P is one candidate for the mediation of the inflammatory response since it is thought to be a neurotransmitter in sensory afferents and since exogenous substance P is capable of eliciting a response characteristic of inflammation. In rabbits, intravitreal or topical application onto the eye of a specific substance P antagonist, [d-Pro2, D-Trp7,9]SP, inhibited not only the irritant effects of exogenous substance P but also the inflammatory response to a standardized trauma (infrared irradiation of the iris). These observations suggest that substance P, or a related peptide, is a neurogenic mediator of the inflammatory response in the eye.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Holmdahl, G -- Hakanson, R -- Leander, S -- Rosell, S -- Folkers, K -- Sundler, F -- New York, N.Y. -- Science. 1981 Nov 27;214(4524):1029-31.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6171036" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Eye Diseases/*drug therapy ; Inflammation/*drug therapy ; Infrared Rays ; Pupil/drug effects/radiation effects ; Rabbits ; Structure-Activity Relationship ; Substance P/*analogs & derivatives/*antagonists & inhibitors/therapeutic use
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  • 85
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    Two distinct central serotonin receptors with different physiological functions (1981)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1981-05-15
    Description: Two distinct serotonin (5-hydroxytryptamine) receptors designated serotonin 1 and serotonin 2 bind tritium-labeled serotonin and tritium-labeled spiroperidol, respectively. Drug potencies at serotonin 2 sites, but not at serotonin 1 sites, predict their effects on the "serotonin behavioral syndrome," indicating that serotonin 2 sites mediate these behaviors. The limited correlation of drug effects with regulation by guanine nucleotides suggests that serotonin 1 sites might be linked to adenylate cyclase. Drug specificities of serotonin-elicited synaptic inhibition and excitation may reflect serotonin 1 and serotonin 2 receptor interactions, respectively.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Peroutka, S J -- Lebovitz, R M -- Snyder, S H -- DA-00074/DA/NIDA NIH HHS/ -- New York, N.Y. -- Science. 1981 May 15;212(4496):827-9.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7221567" target="_blank"〉PubMed〈/a〉
    Keywords: Adenylyl Cyclases/metabolism ; Animals ; Behavior, Animal/*physiology ; Brain/*physiology ; Guanine Nucleotides/physiology ; Kinetics ; Male ; Rats ; Receptors, Serotonin/*physiology ; Serotonin/metabolism ; Spiperone/metabolism ; Structure-Activity Relationship
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  • 86
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    Vasopressin analogs that antagonize antidiuretic responses by rats to the antidiuretic hormone (1981)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1981-04-03
    Description: Four new synthetic analogs of vasopressin (antidiuretic hormone) can antagonize the antidiuretic response to intravenous vasopressin in anesthetized, water-loaded rats. They also cause a diuresis resembling that of diabetes insipidus when given intraperitoneally to conscious rats. Such antagonists may prove to be useful both pharmacologically and therapeutically.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Sawyer, W H -- Pang, P K -- Seto, J -- McEnroe, M -- Lammek, B -- Manning, M -- AM 01940/AM/NIADDK NIH HHS/ -- GM 25280/GM/NIGMS NIH HHS/ -- HL 12738/HL/NHLBI NIH HHS/ -- New York, N.Y. -- Science. 1981 Apr 3;212(4490):49-51.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7209515" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Arginine Vasopressin/*analogs & derivatives/chemical synthesis/pharmacology ; Diuresis/*drug effects ; Female ; Osmolar Concentration ; Rats ; Structure-Activity Relationship ; Vasopressins/*antagonists & inhibitors
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  • 87
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    Angiogenesis inhibition and tumor regression caused by heparin or a heparin fragment in the presence of cortisone (1983)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1983-08-19
    Description: Heparin or a heparin fragment administered with cortisone inhibited angiogenesis, caused regression of large tumor masses, and prevented metastases. Oral administration of heparin resulted in the release of non-anticoagulant heparin fragments in the serum which, in the presence of cortisone, had similar anti-angiogenic and antitumor effects. Of all the heparin fragments tested, the most potent inhibition of angiogenesis in the presence of cortisone was provided by a hexasaccharide with a molecular weight of about 1600.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Folkman, J -- Langer, R -- Linhardt, R J -- Haudenschild, C -- Taylor, S -- EY04002/EY/NEI NIH HHS/ -- GM25810/GM/NIGMS NIH HHS/ -- R01-CA14019/CA/NCI NIH HHS/ -- New York, N.Y. -- Science. 1983 Aug 19;221(4612):719-25.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6192498" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; *Antineoplastic Agents ; Chick Embryo ; Cortisone/*pharmacology ; Heparin/*pharmacology ; Inflammation ; Neoplasm Metastasis ; Neoplasms, Experimental/blood supply ; Neovascularization, Pathologic/*physiopathology ; Oligosaccharides/pharmacology ; Rabbits ; Structure-Activity Relationship
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  • 88
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    Ranking carcinogens for regulation (1983)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1983-01-21
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Crump, K S -- New York, N.Y. -- Science. 1983 Jan 21;219(4582):236-8.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6849134" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Carcinogens/*administration & dosage ; Dose-Response Relationship, Drug ; Humans ; Models, Biological
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  • 89
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    Methadone conformation and opioid activity (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-04-22
    Description: The inactive methadone analog threo-5-methylmethadone has a solid-state conformation in which the nitrogen is antiperiplanar to the tertiary carbon C(4). Since threo-5-methylmethadone exhibits no opioid agonism either in vivo or in vitro, methadone analogs probably do not have this conformation when bound to an opioid receptor. The potent agonist (-)-erythro-5-methylmethadone has a solid-state conformation in which the nitrogen atom is rotated back toward the phenyl rings on the quarternary carbon, suggesting that this unusual conformation is the active one.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Duax, W L -- Smith, G D -- Griffin, J F -- Portoghese, P S -- RR-05716/RR/NCRR NIH HHS/ -- New York, N.Y. -- Science. 1983 Apr 22;220(4595):417-8.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6301007" target="_blank"〉PubMed〈/a〉
    Keywords: Methadone/analogs & derivatives/*pharmacology ; Molecular Conformation ; Receptors, Opioid/metabolism ; Stereoisomerism ; Structure-Activity Relationship
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  • 90
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    Asymmetry of the acetylcholine channel revealed by quaternary anesthetics (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-10-10
    Description: Tissue-cultured rat myoballs were examined electrophysiologically with a suction pipette, which was used for voltage clamping and internal perfusion. The lidocaine derivative QX-314 caused a time- and membrane potentia-dependent block of acetylcholine-induced current only when applied from the extracellular membrane surface. The same compounds caused a use-dependent block of the sodium channel only from the intracellular membrane surface. These experiments demonstrate a fundamental asymmetry of the acetylcholine receptor-channel complex.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Horn, R -- Brodwick, M S -- Dickey, W D -- CA-19017/CA/NCI NIH HHS/ -- NS-12961/NS/NINDS NIH HHS/ -- NS-13778/NS/NINDS NIH HHS/ -- New York, N.Y. -- Science. 1980 Oct 10;210(4466):205-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6251552" target="_blank"〉PubMed〈/a〉
    Keywords: Acetylcholine/*metabolism ; Animals ; *Ion Channels/drug effects ; Lidocaine/*analogs & derivatives/pharmacology ; Membrane Potentials/drug effects ; Membrane Proteins ; Motor Endplate/*ultrastructure ; Neuromuscular Junction/*ultrastructure ; Rats ; *Receptors, Cholinergic ; Sodium/metabolism ; Structure-Activity Relationship
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  • 91
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    Angiotoxicity of oxygenated sterols and possible precursors (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-02-08
    Description: Cell death, inflammation, and repair in rabbits' aortas and pulmonary arteries were observed at 3-, 7-, and 10-day periods after the intravenous injection of oxygenated sterols. Thus, oxygenated sterols, not cholesterol, may play the primary role in arterial wall injury and lesion development.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Imai, H -- Werthessen, N T -- Subramanyam, V -- LeQuesne, P W -- Soloway, A H -- Kanisawa, M -- New York, N.Y. -- Science. 1980 Feb 8;207(4431):651-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7352277" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Aorta/drug effects ; Blood Vessels/*drug effects/pathology ; Cholesterol/*analogs & derivatives/toxicity ; Epoxy Compounds/*toxicity ; Ethers, Cyclic/*toxicity ; Female ; Hydroxycholesterols/toxicity ; Lanosterol/analogs & derivatives/toxicity ; Male ; Necrosis ; Oxidation-Reduction ; Pulmonary Artery/drug effects ; Rabbits ; Structure-Activity Relationship
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  • 92
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    Role of nitrogen dioxide in the biosynthesis of nitraosamines in mice (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-03-28
    Description: Groups of three to four mice were gavaged with aqueous solutions of 2 milligrams of morpholine, after which they were exposed to nitrogen dioxide in inhalation chambers at concentrations of 0.2 to 50 parts per million for up to 4 hours. At sequential intervals during the exposure, mice were frozen and pulverized in liquid nitrogen, and the mice powder was extracted with ice-cold 35 percent aqueous methanol and dichloromethane; organic-phase concentrates were analyzed for N-nitrosomorpholine with a thermal energy analyzer interfaced to a gas chromatograph. The N-nitrosomorpholine yields, ranging up to about 2.3 micrograms per mouse, were time-dependent relative to the duration of exposure to nitrogen dioxide and dose-dependent relative to the concentrations of nitrogen dioxide; control levels (in mice that were gavaged with morpholine or distilled water and then exposed to air instead of nitrogen dioxide) were less than 5 nanograms per mouse. These preliminary studies demonstrate the in vivo nitrosating potential of nitrogen oxides.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Iqbal, Z M -- Dahl, K -- Epstein, S S -- New York, N.Y. -- Science. 1980 Mar 28;207(4438):1475-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7361099" target="_blank"〉PubMed〈/a〉
    Keywords: Amines/metabolism ; Animals ; Ascorbic Acid/pharmacology ; Biotransformation ; Dose-Response Relationship, Drug ; Mice ; Morpholines/*metabolism ; Nitrogen Dioxide/antagonists & inhibitors/*metabolism ; Nitrosamines/*metabolism ; Time Factors
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  • 93
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    Specific locus mutations induced in somatic cells of rats by orally and parenterally administered procarbazine (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-07-11
    Description: A new test, the granuloma pouch assay, was used in detecting specific locus mutations in somatic cells of rats in vivo after the animals were treated orally and parenterally with procarbazine hydrochloride, an agent used in cancer chemotherapy. The results indicate that stable intermediates are formed in the body and distributed as proximate mutagens.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Maier, P -- Zbinden, G -- New York, N.Y. -- Science. 1980 Jul 11;209(4453):299-301.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7384804" target="_blank"〉PubMed〈/a〉
    Keywords: Administration, Oral ; Animals ; Dose-Response Relationship, Drug ; Granulation Tissue/physiopathology ; Injections, Intraperitoneal ; Injections, Intravenous ; Mutation/*drug effects ; Procarbazine/administration & dosage/*pharmacology ; Rats
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  • 94
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    Beta-lipotropin: a new aldosterone-stimulating factor (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-07-11
    Description: Beta-Lipotropin stimulated the production of aldosterone in collagenase-dispersed rat adrenal capsular cells. The maximum response obtained with beta-lipotropin was the same as the response obtained with corticotropin and was greater than that obtained with angiotensin II. These data suggest that beta-lipotropin may play a role in aldosterone regulation.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Matsuoka, H -- Mulrow, P J -- Li, C H -- New York, N.Y. -- Science. 1980 Jul 11;209(4453):307-8.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6247763" target="_blank"〉PubMed〈/a〉
    Keywords: Adrenal Glands/drug effects/*metabolism ; Adrenocorticotropic Hormone/pharmacology ; Aldosterone/*biosynthesis ; Animals ; Corticosterone/*biosynthesis ; Dose-Response Relationship, Drug ; Female ; Rats ; Sheep ; Swine ; beta-Lipotropin/*pharmacology
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  • 95
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    Effect of interferon-alpha 1 from E. coli on some cell functions (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-09-19
    Description: Interferon-alpha 1 from Escherichia coli transformed with a hybrid plasmid containing a human leukocyte complementary DNA insert, induces resistance to virus in appropriate target cells. It also shares the following properties with natural leukocyte interferon (IFN). (i) It enhances natural killing activity of human lymphocytes, (ii) it enhances antibody-dependent cell-mediated cytotoxicity, (iii) it suppresses antigen- and mitogen-induced leukocyte migration inhibition, (iv) it inhibits growth of IFN-sensitive Burkitt lymphoma cells. Since these activities are exhibited by a cloned protein species, they are due to IFN itself and not to other human proteins.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Masucci, M G -- Szigeti, R -- Klein, E -- Klein, G -- Gruest, J -- Montagnier, L -- Taira, H -- Hall, A -- Nagata, S -- Weissmann, C -- New York, N.Y. -- Science. 1980 Sep 19;209(4463):1431-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6158096" target="_blank"〉PubMed〈/a〉
    Keywords: Antibody-Dependent Cell Cytotoxicity/drug effects ; Cell Division/drug effects ; Cell Migration Inhibition ; Cloning, Molecular ; *DNA, Recombinant ; Escherichia coli ; Humans ; Hypersensitivity, Delayed/immunology ; Immunity, Cellular/drug effects ; Interferons/genetics/*pharmacology ; Structure-Activity Relationship
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  • 96
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    At least three human type alpha interferons: structure of alpha 2 (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-09-19
    Description: The sequence of a human leukocyte-derived complementary DNA (cDNA), Hif-2h, which directs the formation in Escherichia coli of a polypeptide, IFN-alpha 1, with interferon (IFN) activity has been described. A second IFN cDNA, Hif-SN206, which also elicits synthesis of a biologically active IFN, IFN-alpha 2, is described in this article. Whereas IFN-alpha 2 is twice as active on human as on bovine cells, IFN-alpha 1 is 10 to 20 times more active on bovine than on human cells. As deduced from the cDNA's, the messenger RNA's for the two IFN's differ in length and in 20 percent of the nucleotides; the mature IFN polypeptides differ in 17 percent of the amino acids. Both IFN-alpha 1 and IFN-alpha 2 differ from the lymphoblastoid IFN described by others. Therefore, at least three different IFN-alpha genes are expressed in man; studies on genomic DNA reveal the presence of at least eight IFN-related genes.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Streuli, M -- Nagata, S -- Weissmann, C -- New York, N.Y. -- Science. 1980 Sep 19;209(4463):1343-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6158094" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Animals ; Base Sequence ; DNA, Recombinant ; Escherichia coli/genetics ; Genes ; Humans ; *Interferons/genetics ; Leukocytes ; Lymphocytes ; Mice ; RNA, Messenger/genetics ; Structure-Activity Relationship
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  • 97
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    DNA methylation and gene function (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-11-07
    Description: In most higher organisms, DNA is modified after synthesis by the enzymatic conversion of many cytosine residues to 5-methylcytosine. For several years, control of gene activity by DNA methylation has been recognized as a logically attractive possibility, but experimental support has proved elusive. However, there is now reason to believe, from recent studies, that DNA methylation is a key element in the hierarchy of control mechanisms that govern vertebrate gene function and differentiation.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Razin, A -- Riggs, A D -- GM20483/GM/NIGMS NIH HHS/ -- GM25825/GM/NIGMS NIH HHS/ -- New York, N.Y. -- Science. 1980 Nov 7;210(4470):604-10.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6254144" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cell Differentiation ; DNA/*physiology ; DNA (Cytosine-5-)-Methyltransferase/*metabolism ; DNA Restriction Enzymes/metabolism ; Deoxycytosine Nucleotides/*metabolism ; Deoxyribonucleoproteins/metabolism ; Gene Expression Regulation ; Methylation ; Methyltransferases/*metabolism ; Nucleosomes/ultrastructure ; Protein Binding ; Structure-Activity Relationship ; Substrate Specificity ; Tissue Distribution
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  • 98
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    War gases as olfactory probes (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-10-01
    Description: The tear gas ethyl bromoacetate is a fruity-smelling alkylating agent that blocks the ability of the frog nose to respond to esters and a variety of other odorants, but leaves sensitivity to amines unimpaired. Lachrymators and chemical warfare agents of other functional types such as sulfides (mustard gas) and amines (nitrogen mustards) may have similarly specific actions that will enable their use as chemical probes of the sense of smell.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Criswell, D W -- McClure, F L -- Schaefer, R -- Brower, K R -- New York, N.Y. -- Science. 1980 Oct;210(4468):425-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6968976" target="_blank"〉PubMed〈/a〉
    Keywords: Alkylating Agents/*pharmacology ; Amines ; Animals ; Chemical Warfare Agents/*pharmacology ; Esters ; Membrane Potentials/drug effects ; Rana pipiens ; Smell/*drug effects/physiology ; Structure-Activity Relationship
    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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    Factors influencing the inhibitory effect of selenium on mice inoculated with Ehrlich ascites tumor cells (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-08-15
    Description: Selenium, administered to mice with Ehrlich ascites tumors, effectively limited tumor growth. The response was dependent on the chemical form and dose of selenium administered. At the doses administered, there were no detectable adverse effects to the host.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Greeder, G A -- Milner, J A -- New York, N.Y. -- Science. 1980 Aug 15;209(4458):825-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7406957" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Carcinoma, Ehrlich Tumor/*drug therapy/pathology ; Cell Line ; Cell Membrane Permeability ; Cystine/analogs & derivatives ; Dose-Response Relationship, Drug ; Male ; Mice ; Neoplasm Transplantation ; Selenium/*administration & dosage/metabolism/therapeutic use ; Selenomethionine/administration & dosage
    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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    Calmodulin plays a pivotal role in cellular regulation (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-01-04
    Description: The role of calcium ions (Ca2+) in cell function is beginning to be unraveled at the molecular level as a result of recent research on calcium-binding proteins and particularly on calmodulin. These proteins interact reversibly with Ca2+ to form a protein . Ca2+ complex, whose activity is regulated by the cellular flux of Ca2+. Many of the effects of Ca2+ appear to be exerted through calmodulin-regulated enzymes.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Cheung, W Y -- New York, N.Y. -- Science. 1980 Jan 4;207(4426):19-27.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6243188" target="_blank"〉PubMed〈/a〉
    Keywords: 3',5'-Cyclic-AMP Phosphodiesterases/metabolism ; Allosteric Regulation ; Amino Acid Sequence ; Animals ; Biological Evolution ; Calcium/*physiology ; Calcium-Binding Proteins/*physiology ; Calmodulin/*physiology ; Cell Communication ; Cyclic AMP/*physiology ; Enzyme Activation ; Phospholipases A/metabolism ; Protein Kinases/*metabolism ; Receptors, Drug/physiology ; Structure-Activity Relationship ; Troponin/physiology
    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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