Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors

被引：9
|
作者：
Wei, ZL
Xiao, YX
Kellar, KJ
Kozikowski, AP
机构：
[1] Univ Illinois, Coll Pharm, Dept Med Chem & Pharmacognosy, Chicago, IL 60612 USA
[2] Georgetown Univ, Dept Pharmacol, Washington, DC 20057 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 08期
关键词：
D O I：
10.1016/j.bmcl.2003.10.071
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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 alpha3beta4 nAChR as shown by functional assays. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1855 / 1858
页数：4
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