High affinity ligands for the α7 nicotinic receptor that show no cross-reactivity with the 5-HT3 receptor

被引：11
|
作者：
Baker, SR [1 ]
Boot, J [1 ]
Brunavs, M [1 ]
Dobson, D [1 ]
Green, R [1 ]
Hayhurst, L [1 ]
Keenan, M [1 ]
Wallace, L [1 ]
机构：
[1] Eli Lilly & Co, Lilly Res Ctr Ltd, Windlesham GU20 6PH, Surrey, England
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 21期
关键词：
D O I：
10.1016/j.bmcl.2005.07.070
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Potent and selective ligands of the alpha 7 nicotinic acetylcholine receptor are required to understand the pharmacological effect of alpha 7 activation. A common cross-reactivity occurs with serotonergic 5-HT3 receptors with which alpha 7 receptors have a high sequence homology. We demonstrate that certain quinuclidine 3-biaryl carboxamides are high affinity a7 ligands with an excellent binding selectivity over 5-HT3 receptors. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4727 / 4730
页数：4
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