Ulixacaltamide

Ulixacaltamide (Z944) is an orally available T-type calcium channel antagonist that can slow the progression of epilepsy. Ulixacaltamide effectively reduces tremor in a normal alkaline tremor animal model. Ulixacaltamide reverses thermal hyperalgesia and mediates pain relief^[1][2][3][4]. In Vitro: Ulixacaltamide (1 μM) inhibits the whole-cell current amplitude of transiently expressed human Cav3.2 calcium channels by approximately 50% (IC₅₀=0.60 μM)^[4].
Ulixacaltamide (10 μM) abolishs completely the transient current component generated by depolarization to 30 mV after activation of T-type calcium channels, reducing the whole-cell calcium current of tsA-201 cells by approximately 70%^[4].
In Vivo: Ulixacaltamide (5, 10, 30 and 100 mg/kg; i.p.; single dose) delaies the development of fully induced epilepsy in mice at a dose of 30 mg/kg, requiring more stimulations to induce type III, IV or V seizures^[2].
Ulixacaltamide (0.1-3 mg/kg; p.o.) dose-dependently reduces the frequency of harmaline-induced tremors in rats^[3].
Ulixacaltamide (10 mg/kg; i.p.; single dose) effectively reverses the thermal hypersensitivity response induced by Complete Freund's adjuvant (CFA) (HY-153808) in male C57BL mice, with the analgesic effect reaching a peak at 90 minutes after injection^[4].