PubMed 18243692
Referenced in: none
Automatically associated channels: Nav1.7
Title: Imidazopyridines: a novel class of hNav1.7 channel blockers.
Authors: Clare London, Scott B Hoyt, William H Parsons, Brande S Williams, Vivien A Warren, Richard Tschirret-Guth, McHardy M Smith, Birgit T Priest, Erin McGowan, William J Martin, Kathryn A Lyons, Xiaohua Li, Bindhu V Karanam, Nina Jochnowitz, Maria L Garcia, John P Felix, Brian Dean, Catherine Abbadie, Gregory J Kaczorowski, Joseph L Duffy
Journal, date & volume: Bioorg. Med. Chem. Lett., 2008 Mar 1 , 18, 1696-701
PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/18243692
Abstract
A series of imidazopyridines were evaluated as potential sodium channel blockers for the treatment of neuropathic pain. Several members were identified with good hNa(v)1.7 potency and excellent rat pharmacokinetic profiles. Compound 4 had good efficacy (52% and 41% reversal of allodynia at 2 and 4h post-dose, respectively) in the Chung rat spinal nerve ligation (SNL) model of neuropathic pain when dosed orally at 10mg/kg.