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J Med Chem. 2008 May 22;51(10):2887-90. doi: 10.1021/jm8001444. Epub 2008 Apr 24.

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

Author information

1
Psychiatry Centre of Excellence for Drug Discovery and Molecular Discovery Research, GlaxoSmithKline, Essex, UK. Simon.E.Ward@gsk.com

Abstract

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.

PMID:
18433113
DOI:
10.1021/jm8001444
[Indexed for MEDLINE]

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