Discovery of Potent, Orally Bioavailable, Selective 5-HT1A/B/D Receptor Antagonists

Journal of Medicinal Chemistry
2008.0

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.

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