2-aryl tryptamines:: Selective high-affinity antagonists for the h5-HT2A receptor

被引：75

作者：

Stevenson, GI ^{[1
]}

Smith, AL ^{[1
]}

Lewis, S ^{[1
]}

Michie, SG ^{[1
]}

Neduvelil, JG ^{[1
]}

Patel, S ^{[1
]}

Marwood, R ^{[1
]}

Patel, S ^{[1
]}

Castro, JL ^{[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)00557-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2-aryl tryptamines have been identified as high-affinity h6-HT2A antagonists. Structure-activity relationship studies have shown that h5-HT2A affinity can be attained via modifications to the tryptamine side chain and that selectivity over h5-HT2C and hD(2) receptors can be controlled by suitable C-2 aryl groups. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2697 / 2699

页数：3

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