Painful research: identification of a small-molecule inhibitor that selectively targets Nav1.8 sodium channels.
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.
Rush
Anthony M
AM
NeuroSolutions Ltd., Coventry CV4 7ZS, UK. TRush@neurosolutionsltd.com
Cummins
Theodore R
TR
D000814:Aniline Compounds / Q000378:metabolism / Q000627:therapeutic use; D000818:Animals; D005663:Furans / Q000378:metabolism / Q000627:therapeutic use; D006801:Humans; D062559:NAV1.8 Voltage-Gated Sodium Channel; D009474:Neurons / Q000378:metabolism; D009619:Nociceptors / Q000378:metabolism; D010146:Pain / Q000188:drug therapy*; D020033:Protein Isoforms / Q000235:genetics / Q000378:metabolism; D026941:Sodium Channel Blockers / Q000378:metabolism / Q000627:therapeutic use; D015222:Sodium Channels / Q000235:genetics / Q000378:metabolism*