Dibenzazepines and dibenzoxazepines as sodium channel blockers

Bioorg Med Chem Lett. 2015 Jan 1;25(1):43-7. doi: 10.1016/j.bmcl.2014.11.025. Epub 2014 Nov 14.

Abstract

We have identified two related series of dibenzazepine and dibenzoxazepine sodium channel blockers, which showed good potency on Nav1.7 in FLIPR-based and electrophysiological functional assays.

MeSH terms

  • Animals
  • Dibenzazepines / chemistry*
  • Dibenzazepines / pharmacology
  • Dibenzoxazepines / chemistry*
  • Dibenzoxazepines / pharmacology
  • Humans
  • Microsomes, Liver / drug effects
  • Microsomes, Liver / physiology
  • NAV1.7 Voltage-Gated Sodium Channel / physiology*
  • Rats
  • Sodium Channel Blockers / chemistry*
  • Sodium Channel Blockers / pharmacology

Substances

  • Dibenzazepines
  • Dibenzoxazepines
  • NAV1.7 Voltage-Gated Sodium Channel
  • Sodium Channel Blockers
  • dibenzazepine