Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors.
Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors.
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神经元烟碱乙酰胆碱受体的皮巴替丁二价配体的合成和药理学表征。
DOI：
10.1016/j.bmcl.2003.10.071
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发表时间：
2004
影响因子：
2.7
通讯作者：
Kozikowski,AlanP
中科院分区：
文献类型：
--
作者：
Wei,Zhi-Liang;Xiao,Yingxian;Kellar,KennethJ;Kozikowski,AlanP
A series of bivalent ligands 6a–d of epibatidine were synthesized. All four ligands showed nanomolar binding affinities at six neuronal nicotinic acetylcholine receptor (nAChR) subtypes in competition binding assays. In contrast to epibatidine, these bivalent ligands are weak partial agonists at the α3β4 nAChR as shown by functional assays.
