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Vernier JM, Holsenback H, Cosford ND, Whitten JP, Menzaghi F, Reid R, Rao TS, Sacaan AI, Lloyd GK, Suto CM, Chavez-Noriega LE, Washburn MS, Urrutia A, McDonald IA: Conformationally restricted analogues of nicotine and anabasine. . Bioorg Med Chem Lett. 1998 Aug 18;8(16):2173-8.
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. |
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