A-803467

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Description

A-803467 is a potent and selective Nav1.8 sodium channel blocker. A-803467 blocks Nav1.8 in both half-maximal inactive and resting states with an IC50 of 8 nM and IC50 of 79 nM, respectively. A-803467 is >100-fold selective vs. human Na(v)1.2, Na(v)1.3, Na(v)1.5, and Na(v)1.7 (IC50 values >or=1 microM). Administration of A-803467 (10-30 mg/kg i.v.) reduced mechanically evoked (10-g von Frey hair) and spontaneous WDR neuronal activity in SNL rats. A-803467 also dose-dependently reduced mechanical allodynia in a variety of rat pain models. A-803467 is the first small-molecule blocker of sodium channels which showing both high potency and significant subtype-selectivity among the sodium channel family.

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