Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits.
Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits.
复制标题
DOI：
10.1021/jm0492406
复制
发表时间：
2005-03
影响因子：
7.3
通讯作者：
Zhi-Liang Wei;Yingxian Xiao;Hongbin Yuan;Maryna Baydyuk;P. Petukhov;J. Musachio;K. Kellar;A. Kozikowski
中科院分区：
文献类型：
--
作者：
Zhi-Liang Wei;Yingxian Xiao;Hongbin Yuan;Maryna Baydyuk;P. Petukhov;J. Musachio;K. Kellar;A. Kozikowski
Introduction of a hydrophobic or hydrogen-bonding alkynyl group into the C5 position of the pyridyl ring of epibatidine and A-84543 significantly increased the selectivity for neuronal nicotinic acetylcholine receptors (nAChRs) containing beta2 subunits over nAChRs containing beta4 subunits (K(i) ratio up to 92000-fold). Our data indicate that the extracellular domains of the nAChRs are sufficiently different to allow for the design of novel ligands with high affinity and selectivity for the nAChR subtypes.
