Biological Activity 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 peak currents at all voltages and stimulates a persistent Na+ current at hNav1.7 channel. Increases hyperpolarization at Nav1.4 and Nav1.6 channels. Induces spontaneous pain in vivo.
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