Homotryptamines as potent and selective serotonin reuptake inhibitors (SSRIs)

被引：22

作者：

Schmitz, WD ^{[1
]}

Denhart, DJ ^{[1
]}

Brenner, AB ^{[1
]}

Ditta, JL ^{[1
]}

Mattson, RJ ^{[1
]}

Mattson, GK ^{[1
]}

Molski, TF ^{[1
]}

Macor, JE ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Wallingford, CT 06492 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 06期

关键词：

homotryptamines; SSRI; serotonin reuptake;

D O I：

10.1016/j.bmcl.2005.01.059

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of N,N-dimethylhomotryptamines was prepared and their binding affinities at the serotonin transporter (SERT) were determined. Compounds possessing an electron withdrawing substituent at the C5-position of the indole nucleus were found to be potent SSRIs. Initial attempts at conformational restriction of the propylamine sidechain by incorporation of a quinuclidine bicyclic structure did not improve binding affinity at SERT. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：1619 / 1621

页数：3

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