The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective α7 nicotinic receptor partial agonist

被引：143

作者：

Macor, JE ^{[1
]}

Gurley, D ^{[1
]}

Lanthorn, T ^{[1
]}

Loch, J ^{[1
]}

Mack, RA ^{[1
]}

Mullen, G ^{[1
]}

Tran, O ^{[1
]}

Wright, N ^{[1
]}

Gordon, JC ^{[1
]}

机构：

[1] Three Biotech, AstraZeneca, Worcester, MA 01605 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 03期

关键词：

D O I：

10.1016/S0960-894X(00)00670-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The 5-HT3 receptor antagonist tropisetron (ICS 205-930) was found to be a potent and selective partial agonist at alpha7 nicotinic receptors. Two other 5-HT3 receptor antagonists, ondansetron and LY-278,584. were found to lack high affinity at the alpha7 nicotinic receptor. Quinuclidine analogues (1 and 2) of tropisetron were also found to be potent and selective partial agonists at alpha7 nicotinic receptors. (C) 2001 Elsevier Science Ltd. All rights reserved.

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页码：319 / 321

页数：3

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