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Updated: Jul 11, 2026

Method for Identifying Small Molecule Inhibitors of the Protein-protein Interaction Between HCN1 and TRIP8b
Published on: November 11, 2016
Painful research: identification of a small-molecule inhibitor that selectively targets Nav1.8 sodium channels
Anthony M Rush1, Theodore R Cummins
1NeuroSolutions Ltd., Coventry CV4 7ZS, UK. TRush@neurosolutionsltd.com
Abstract:
Voltage-gated sodium channels in nociceptive neurons are attractive targets for novel pain therapeutics. Although drugs that target voltage-gated sodium channels have proven value as pain therapeutics, the drugs that are currently available are non-specific sodium channel inhibitors, which limit their usefulness. Recently, a selective small-molecule inhibitor of Na(v)1.8, a voltage-gated sodium channel isoform that participates in peripheral pain mechanisms, has been developed. This exciting new compound shows efficacy in several animal models of pain and is anticipated to be only the first of many new isoform-specific sodium channel blockers.
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