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Apinocaltamide

CAS No. : 1838651-58-3

MCE 站：Apinocaltamide

产品活性：Apinocaltamide (ACT-709478) 是一种口服有效的，可透过血脑屏障的选择性 T 型电压门控钙通道 (T-type calcium channel) 阻滞剂，可用于全身性癫痫的研究。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：Calcium Channel

In Vitro: Apinocaltamide (Compound 66b) blocks Ca_v3.1, Ca_v3.2, Ca_v3.3, Ca_v1.2 with IC₅₀s of 6.4, 18, 7.5 ａnd 2410 nM, respectively. Apinocaltamide blocks recombinant channel hCa_v3.3 potently with marked voltage-dependency (K_r≈1500 nM ａnd K_i≈20 nM). Apinocaltamide blocks currents through hK_v11.1-hERG channels with an IC₅₀ of 5.5 μM.
Apinocaltamide also inhibits P450 enzymes with IC₅₀s of 14, 15, 22, 25, 51 ａnd 52 μM for CYP2C8,CYP2D6 CYP2C9, CYP2C19, CYP3A4, ａnd CYP2B6, respectively.

In Vivo: Apinocaltamide (Compound 66b, 100, 300 mg/kg, p.o., measured 12 hours later) potently decreases the cumulative duration of absence-like seizures in mice.

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