tcsc0014686 Cenobamate

Cenobamate, a sodium channel blocker, enhances GABAergic transmission and has the potential to be a versatile CNS drug.

IC50 & Target: Sodium channel, GABA receptor^[1].

In Vivo: Cenobamate (YKP3089) protects against MES induced seizures in mice with an ED₅₀ of 9.8 mg/kg i.p., and in rats with an ED₅₀ of 1.9 mg/kg p.o. In the sc Met seizures model, Cenobamate given ip inhibited the clonic seizures in mice and rats, with ED₅₀ values of 28.5 and 13.6 mg/kg, respectively. Cenobamate is also effective against seizure induced by picrotoxin with an ED₅₀ of 34.5 mg/kg in mice. Cenobamate is effective in reducing significantly the expression of stage 5 seizures in the hippocampal kindled rat (ED₅₀=16.4 mg/kg). Cenobamate is effective in the mouse 6 Hz psychomotor seizure model at 22, 32 and 44 mA, with ED₅₀ values of 11.0, 17.9 and 16.5 mg/kg, respectively. Cenobamate also protects against lithiumpilocarpine-induced intractable seizures in rats (ip) (ED₅₀=7.0 mg/kg)^[2].