Studies towards the next generation of antidepressants.: Part 4:: Derivatives of 4-(5-fluoro-1H-indol-3-yl)cyclohexylamine with affinity for the serotonin transporter and the 5-HT1A receptor

被引：28

作者：

Evrard, DA

Zhou, P

Yi, SY

Zhou, DH

Smith, DL

Sullivan, KM

Hornby, GA

Schechter, LE

Andree, TH

Mewshaw, RE

机构：

[1] Wyeth Ayerst Res, Chem & Screening Sci, Princeton, NJ 08543 USA

[2] Wyeth Ayerst Res, Neurosci Discovery Res, Princeton, NJ 08543 USA

[3] Wyeth Ayerst Res, Chem & Screening Sci, Collegeville, PA 19426 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 04期

关键词：

serotonin; SSRI; 5-HT1A receptor antagonist; antidepressant;

D O I：

10.1016/j.bmcl.2004.12.064

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Derivatives of the serotonin reuptake inhibitor 4-(5-fluoro-1H-indol-3-yl)cyclohexylamine, in which serotonin 1A (5-HT1A) receptor pharmacophoric elements are incorporated, are reported. Analogs exhibiting affinity for both the serotonin transporter and the 5-HT1A receptor are described. Compounds containing 1-(4-indolyl)piperazine and 2-(1H-indol-4-yloxy)ethylamine are promising leads for further SAR studies. (C) 2005 Elsevier Ltd. All rights reserved.

引用

页码：911 / 914

页数：4

共 32 条

[1] Acceleration of the effect of selected antidepressant drugs in major depression by 5-HT1A antagonists [J].