Potent rat Nav1.7, human Nav1.4 and rat Nav1.6 channel activator (EC50 values are 7, 10 and 47 nM, respectively). Exhibits minimal activation at mammalian Nav1.2, Nav1.3 and Nav1.5 (EC50 values >3 μM). Inhibits fast inactivation on all channels. Increases
Potent and reversible Kv3.4 potassium channel blocker (IC50 = 47 nM); also attenuates inactivation of sodium currents by acting on Nav1.7 and Nav1.3 channels. Enhances TTX-sensitive sodium currents in rat small dorsal root ganglion neurons. Neuroprotective.