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 hNav1.7, and was orally efficacious in a rat model of 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 hNav1.7, and was orally efficacious in a rat model of neuropathic pain.Figure optionsDownload as PowerPoint slide