Relutrigine is an orally active sodium current inhibitor that specifically targets persistent sodium channels. It demonstrates potent inhibition of persistent INa induced by both ATX-II (Nav 1.5 activator) and the SCN8A mutation N1768D, with IC50 values of 141 nM and 75 nM, respectively. In addition to exhibiting a strong use-dependent block, Relutrigine effectively reduces intrinsic neuronal excitability and possesses significant anticonvulsant properties, making it valuable for research in neuropharmacology and epilepsy studies.
Relutrigine is an orally active sodium current inhibitor that specifically targets persistent sodium channels. It demonstrates potent inhibition of persistent INa induced by both ATX-II (Nav 1.5 activator) and the SCN8A mutation N1768D, with IC50 values of 141 nM and 75 nM, respectively. In addition to exhibiting a strong use-dependent block, Relutrigine effectively reduces intrinsic neuronal excitability and possesses significant anticonvulsant properties, making it valuable for research in neuropharmacology and epilepsy studies.
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