Discovery of a novel class of benzazepinone Nav1.7 blockers:: Potential treatments for neuropathic pain

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. (c) 2007 Elsevier Ltd. All rights reserved.