Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists

被引：10

作者：

Ward, Simon E. ^{[1
]}

Eddershaw, Peter J. ^{[1
]}

Scott, Claire M. ^{[1
]}

Gordon, Laurie J. ^{[1
]}

Lovell, Peter J. ^{[1
]}

Moore, Susan H. ^{[1
]}

Smith, Paul W. ^{[1
]}

Starr, Kathryn R. ^{[1
]}

Thewlis, Kevin M. ^{[1
]}

Watson, Jeannette M. ^{[1
]}

机构：

[1] GlaxoSmithKline, Psychiat Ctr Excellence Drug Discovery & Mol Disc, Harlow CM19 5AW, Essex, England

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 10期

关键词：

D O I：

10.1021/jm8001444

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

5-HT1 receptor antagonists have been discovered with good selectivity over the 5-HT transporter. This is the first report of highly potent, selective ligands for the 5-HT1A/B/D receptors with low intrinsic activity, which represent a useful set of molecules for further understanding the roles of the 5-HT1 receptor subtypes and providing new approaches,for the treatment of depression.

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收藏

页码：2887 / 2890

页数：4

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