Relutrigine (PRAX-562) is an orally active inhibitor of persistent sodium channel. Relutrigine potently and preferentially inhibits persistent INa induced by ATX-II (Nav 1.5 activator) or the SCN8A mutation N1768D with IC50 values of 141 nM and 75 nM, respectively. Relutrigine exhibits potent use-dependent block and reduces neuronal intrinsic excitability. Relutrigine has effective anticonvulsant activity.

Relutrigine (PRAX-562) 是一种具有口服活性的持久性钠通道 (sodium channel) 抑制剂。Relutrigine 有效且优先抑制 ATX-II (Nav 1.5 激活剂) 或 SCN8A 突变 N1768D 诱导的持续性 INa，IC50 值分别为 141 nM 和 75 nM。Relutrigine 表现出使用依赖性阻滞，降低了神经元的内在兴奋性。Relutrigine 具有有效的抗惊厥活性。