Vernier J M, Holsenback H, Cosford N D, Whitten J P, Menzaghi F, Reid R, Rao T S, Sacaan A I, Lloyd G K, Suto C M, Chavez-Noriega L E, Washburn M S, Urrutia A, McDonald I A
SIBIA Neurosciences Inc., La Jolla, CA 92037, USA.
Bioorg Med Chem Lett. 1998 Aug 18;8(16):2173-8. doi: 10.1016/s0960-894x(98)00394-1.
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.
已合成了一系列尼古丁的构象受限类似物，并将其作为神经元乙酰胆碱受体激动剂进行了评估。化合物2（SIB - 1663）可选择性激活人重组α2β4和α4β4烟碱型乙酰胆碱受体，在帕金森病和疼痛的动物模型中显示出活性。
