Amidine derived inhibitors of acid-sensing ion channel-3 (ASIC3)

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4059-63. doi: 10.1016/j.bmcl.2009.06.021. Epub 2009 Jun 13.

Abstract

A series of indole amidines modified at the 2-position of the indole ring were evaluated as inhibitors of Acid-Sensing Ion Channel-3 (ASIC3), a novel target for the treatment of chronic pain.

MeSH terms

  • Acid Sensing Ion Channels
  • Amidines / chemistry*
  • Animals
  • Chemistry, Pharmaceutical / methods*
  • Drug Design
  • Electrophysiology
  • Indoles / chemistry
  • Inhibitory Concentration 50
  • Ion Channels / chemistry
  • Male
  • Models, Chemical
  • Naproxen / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Sodium Channels / chemistry*
  • Structure-Activity Relationship

Substances

  • ASIC3 protein, human
  • Acid Sensing Ion Channels
  • Amidines
  • Indoles
  • Ion Channels
  • Sodium Channels
  • Naproxen