Description
A potent blocker of Neuronal TTX-Sensitive Voltage-Gated Na+ Channel that preferentially inhibits neuronal voltage-gated sodium channel subtype hNav1.7 (SCN9A) (IC50 = 26 nM), rNav1.2 (SCN2A) (IC50 = 150 nM), and rNav1.3 (SCN3A) (IC50 = 338 nM), compared with muscle subtypes rNav1.4 (SCN4A) and hNav1.5 (SCN5A) (IC50 > 10 µM). Huwentoxin IV inhibits the activation of sodium channels by trapping the voltage sensor of domain II of the site 4 in the inward, closed configuration