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Bioorg Med Chem Lett. 2012 Mar 1;22(5):1870-3. doi: 10.1016/j.bmcl.2012.01.080. Epub 2012 Jan 28.

Identification of fused bicyclic heterocycles as potent and selective 5-HT(2A) receptor antagonists for the treatment of insomnia.

Author information

  • 1Arena Pharmaceuticals Inc., 6166 Nancy Ridge Drive, San Diego, CA 92121, USA. yxiong@arenapharm.com

Abstract

A series of fused bicyclic heterocycles was identified as potent and selective 5-HT(2A) receptor antagonists. Optimization of the series resulted in compounds that had improved PK properties, favorable CNS partitioning, good pharmacokinetic properties, and significant improvements on deep sleep (delta power) and sleep consolidation.

Copyright © 2012 Elsevier Ltd. All rights reserved.

PMID:
22325948
[PubMed - indexed for MEDLINE]
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