A novel benzazepinone sodium channel blocker with oral efficacy in a rat model of neuropathic pain

Bioorg Med Chem Lett. 2013 Jun 15;23(12):3640-5. doi: 10.1016/j.bmcl.2013.03.121. Epub 2013 Apr 5.

Abstract

A series of benzazepinones were synthesized and evaluated for block of Nav1.7 sodium channels. Compound 30 from this series displayed potent channel block, good selectivity versus other targets, and dose-dependent oral efficacy in a rat model of neuropathic pain.

Publication types

  • Letter

MeSH terms

  • Animals
  • Benzazepines / pharmacology*
  • Disease Models, Animal
  • Neuralgia / drug therapy*
  • Rats
  • Sodium Channel Blockers / pharmacology*

Substances

  • Benzazepines
  • Sodium Channel Blockers