3-(4-piperidinyl)- and 3-(8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indoles as bioavailable h5-HT2A antagonists

被引：9

作者：

Crawforth, J ^{[1
]}

Goodacre, S ^{[1
]}

Maxey, R ^{[1
]}

Bourrain, S ^{[1
]}

Patel, S ^{[1
]}

Marwood, R ^{[1
]}

O'Connor, D ^{[1
]}

Herbert, R ^{[1
]}

Hutson, P ^{[1
]}

Rowley, M ^{[1
]}

机构：

[1] Merck Sharp & Dohme Res Labs, Neurosci Res Ctr, Harlow CM20 2QR, Essex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 24期

关键词：

D O I：

10.1016/S0960-894X(00)00559-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 3-(4-piperidinyl)- and 3-(8-aza-bicyclo[3.2.1] oct-3-yl)-2-phenyl-1H-indoles have been prepared and evaluated as ligands for the h5-HT2A receptor. 3-(8-Phenethyl-8-aza-bicyclol[3.2.1]oct-3-yl)-2-phenyl-1H-indole is a high-affinity (1.2 nM), selective (>800 fold over h5-HT2C and hD(2) receptors) antagonist at the h5-HT2A receptor with oral bioavailability in rats. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2701 / 2703

页数：3

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