Biological Activity
Cenobamate, a sodium channel blocker, enhances GABAergic transmission and has the potential to be a versatile CNS drug.
In Vitro
No in vitro data are provided in the current product source. Contact us for further information.
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].
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.