2. Academic Validation
  3. Imidazopyridines: a novel class of hNav1.7 channel blockers

Imidazopyridines: a novel class of hNav1.7 channel blockers

  • Bioorg Med Chem Lett. 2008 Mar 1;18(5):1696-701. doi: 10.1016/j.bmcl.2008.01.047.
Clare London 1,  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
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. clare_london@merck.com
PMID: 18243692 DOI: 10.1016/j.bmcl.2008.01.047
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.

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