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Conformationally restricted analogues of nicotine and anabasine
J M Vernier1, H Holsenback, N D Cosford
1SIBIA Neurosciences Inc., La Jolla, CA 92037, USA.
Bioorganic & Medicinal Chemistry Letters
|January 5, 1999
Abstract:
A series of conformationally restricted analogues of nicotine has been synthesized and evaluated as agonists of neuronal acetylcholine receptors. Compound 2 (SIB-1663), which selectively activated human recombinant alpha 2 beta 4 and alpha 4 beta 4 nAChRs, was shown to be active in animal models of Parkinson's disease and pain.