An inhibitor of T-type calcium channels
ACT-709478 is an inhibitor of T-type voltage-gated calcium channel 3.1 (Cav3.1), Cav3.2, and Cav3.3 (IC50s = 6.4, 18, and 7.5 nM, respectively).1 It is selective for T-type calcium channels over the L-type calcium channel Cav1.2 (IC50 = 2,410 nM). ACT-701478 (10 mg/kg) reduces the cumulative duration of absence-like seizures in rats. It also reduces the severity of seizures in a rat model of audiogenic seizures when administered at a dose of 100 mg/kg.
1.Bezen?on, O., Heidmann, B., Siegrist, R., et al.Discovery of a potent, selective T-type calcium channel blocker as a drug candidate for the treatment of generalized epilepsiesJ. Med. Chem.60(23)9769-9789(2017)
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