Elz, Sigurd and Zimmermann, H. and Rehse, K. (1993) Selectivity of sterically fixed tryptamine and 5-methoxytryptamine derivatives for serotonin receptor subtypes, II: Structure-activity relationships and in vitro pharmacology of N-alkyl- and N,N-dialkyl-3- indolylbicyclo-[2.2.1]-heptane-2-amines. Archiv der Pharmazie 326 (11), pp. 893-899.
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Twenty-four norbornane analogues of tryptamine and 5-methoxytryptamine were investigated for affinity at 5-HT2 receptors of the rat tail artery and proved to be weak non-competitive antagonists of 5-HT. Compound 12 which displayed a marked depression of the concentration-effect curves, was examined for potential interaction with the allosteric binding site of the 5-HT2 receptor. The effects elicited by 12, in the presence and absence of the allosteric activator ketanserin, were atypical and must be attributed to a mechanism, unknown up to now. In radioligand displacement experiments binding data for a set of nine compounds were determined at 5-HT1-like, 5-HT2 and 5-HT3 receptors, indicating subtype selectivity for some analogues. The binding affinity of 8 at 5-HT3 receptors which was comparable with the affinity of the selective 5-HT3 agonist 2-methyl-5-HT, could not be demonstrated on the longitudinal muscle strip of the guinea-pig ileum, partially due to the M3 antimuscarinic activity of 8. Functional studies on the rat oesophageal tunica muscularis mucosae did not reveal 5-HT4 agonist properties for two analogues of 5-methoxytryptamine (8, 16).
|Additional information (public):||Elz, S Zimmermann, H Rehse, K In Vitro Research Support, Non-U.S. Gov't Germany Archiv der Pharmazie Arch Pharm (Weinheim). 1993 Nov;326(11):893-9.|
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz)|
|Keywords:||5-Methoxytryptamine/analogs & derivatives/*chemical synthesis/pharmacology Animals Bicyclo Compounds/*chemical synthesis/pharmacology Female Guinea Pigs Indoles/*chemical synthesis/pharmacology Rats *Serotonin Antagonists Structure-Activity Relationship Tryptamines/*chemical synthesis/pharmacology|
|Subjects:||500 Science > 570 Life sciences|
500 Science > 540 Chemistry & allied sciences
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||No|
|Owner:||Prof. Dr. Sigurd Elz|
|Deposited On:||19 Oct 2010 12:27|
|Last Modified:||19 Oct 2010 12:27|