Publikationsdatum:
1979-06-15
Beschreibung:
Substitution of fluorine for hydrogen in position 2, 5, or 6 of the aromatic ring of norepinephrine markedly alters the alpha- and beta-adrenergic agonist properties of norephinephrine. The 6-fluoro isomer is an beta-adrenergic agonist with virtually no beta agonist activity, while the 2-fluoro isomer is a beta-adrenergic agonist with little alpha activity. The 5-fluoro isomer is equipotent with norepinephrine as an alpha agonist and significantly more potent as a beta agonist. The possible physiochemical basis for these differences is discussed.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Cantacuzene, D -- Kirk, K L -- McCulloh, D H -- Creveling, C R -- New York, N.Y. -- Science. 1979 Jun 15;204(4398):1217-9.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/221978" target="_blank"〉PubMed〈/a〉
Schlagwort(e):
Animals
;
Aorta
;
Fluorine
;
Guinea Pigs
;
Hydrogen Bonding
;
In Vitro Techniques
;
Norepinephrine/*analogs & derivatives/chemical synthesis/pharmacology
;
Receptors, Adrenergic/*drug effects
;
Receptors, Adrenergic, alpha/*drug effects
;
Receptors, Adrenergic, beta/*drug effects
;
Structure-Activity Relationship
Print ISSN:
0036-8075
Digitale ISSN:
1095-9203
Thema:
Biologie
,
Chemie und Pharmazie
,
Informatik
,
Medizin
,
Allgemeine Naturwissenschaft
,
Physik
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