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

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.
AuthorsScott B Hoyt, Clare London, Catherine Abbadie, John P Felix, Maria L Garcia, Nina Jochnowitz, Bindhu V Karanam, Xiaohua Li, Kathryn A Lyons, Erin McGowan, Birgit T Priest, McHardy M Smith, Vivien A Warren, Brande S Thomas-Fowlkes, Gregory J Kaczorowski, Joseph L Duffy
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 23 Issue 12 Pg. 3640-5 (Jun 15 2013) ISSN: 1464-3405 [Electronic] England
PMID23652221 (Publication Type: Letter)
CopyrightCopyright © 2013 Elsevier Ltd. All rights reserved.
Chemical References
  • Benzazepines
  • Sodium Channel Blockers
Topics
  • Animals
  • Benzazepines (pharmacology)
  • Disease Models, Animal
  • Neuralgia (drug therapy)
  • Rats
  • Sodium Channel Blockers (pharmacology)

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