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Bioorg Med Chem Lett. 2007 Aug 15;17(16):4630-4. Epub 2007 May 27.

Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. scott_hoyt@merck.com

Abstract

A series of benzodiazepines and benzazepinones were synthesized and evaluated as potential sodium channel blockers in a functional, membrane potential-based assay. One member of the benzazepinone series, compound 47, displayed potent, state-dependent block of hNa(v)1.7, and was orally efficacious in a rat model of neuropathic pain.

PMID:
17588748
DOI:
10.1016/j.bmcl.2007.05.076
[Indexed for MEDLINE]

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