Channelpedia

PubMed 20709545


Referenced in Channelpedia wiki pages of: none

Automatically associated channels: Nav1.7



Title: Substituted biaryl pyrazoles as sodium channel blockers.

Authors: Sriram Tyagarajan, Prasun K Chakravarty, Bishan Zhou, Brett Taylor, Michael H Fisher, Mathew J Wyvratt, Kathy Lyons, Tracy Klatt, Xiaohua Li, Sanjeev Kumar, Brande Williams, John Felix, Birgit T Priest, Richard M Brochu, Vivien Warren, McHardy Smith, Maria Garcia, Gregory J Kaczorowski, William J Martin, Catherine Abbadie, Erin McGowan, Nina Jochnowitz, William H Parsons

Journal, date & volume: Bioorg. Med. Chem. Lett., 2010 Sep 15 , 20, 5480-3

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/20709545


Abstract
Voltage-gated sodium channels have been shown to play a critical role in neuropathic pain. A series of low molecular weight biaryl substituted pyrazole carboxamides were identified with good in-vitro potency and in-vivo efficacy. Compound 26, a Nav1.7 blocker has excellent efficacy in the Chung model of neuropathic pain.