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Updated: Jul 7, 2026

Method for Identifying Small Molecule Inhibitors of the Protein-protein Interaction Between HCN1 and TRIP8b
Published on: November 11, 2016
Imidazopyridines: a novel class of hNav1.7 channel blockers
Clare London1, Scott B Hoyt, William H Parsons
1Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. clare_london@merck.com
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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