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Synthesis, analgesic activity, and binding properties of some epibatidine analogs with a tropine skeleton.

作者信息

Rádl S, Hafner W, Budesínsky M, Hejnová L, Krejcí I

机构信息

Research Institute of Pharmacy and Biochemistry, Prague, Czech Republic.

出版信息

Arch Pharm (Weinheim). 2000 Jun;333(6):167-74. doi: 10.1002/1521-4184(20006)333:6<167::aid-ardp167>3.0.co;2-8.

DOI:10.1002/1521-4184(20006)333:6<167::aid-ardp167>3.0.co;2-8
PMID:10909188
Abstract

A series of epibatidine analogs and their positional isomers bearing an 8-azabicyclo[3.2.1]octane moiety is described. Also some of their simplified analogs bearing a 3-piperidine moiety are reported. Their receptor binding profiles (5-HT1A, 5-HT1B, M1, M2, neuronal nicotinic receptor) and analgesic activity (hot plate, acetic acid induced writhing) have been studied. Some of the compounds, especially those containing an 8-azabicyclo[3.2.1]oct-2-ene moiety possess high afinity for the nicotinic cholinergic receptor. The most analgesically active compounds are also highly toxic. Optimized structures (PM3-MOPAC, Alchemy 2000, Tripos Inc.) of compounds 1-9 were compared with that of epibatidine.

摘要

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