Retigabine dihydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

瑞替加滨二盐酸盐是一种抗惊厥药，用作有治疗经验的成年患者部分性癫痫的辅助治疗。作用机制涉及打开神经元 K(V)7.2-7.5（以前称为 KCNQ2-5）电压激活的 K(+) 通道。在分化的 PC12 细胞中，瑞替加滨增强了利诺吡啶敏感电流。

Retigabine dihydrochloride is an anticonvulsant used as an adjunctive treatment for partial epilepsies in treatment-experienced adult patients.?The mechanism of action involves opening of neuronal K(V)7.2-7.5 (formerly KCNQ2-5) voltage-activated K(+) channels.In differentiated PC12 cells, retigabine enhanced a linopirdine-sensitive current.?The effect of retigabine was associated with a slowing of M-like tail current deactivation in these cells.?Retigabine (0.1 to 10 microM) induced a potassium current and hyperpolarized CHO cells expressing KCNQ2/Q3 cells but not in wild-type cells.?Retigabine-induced currents in CHO-KCNQ2/Q3 cells were inhibited by 60.6 +/- 11% (n = 4) by the KCNQ2/Q3 blocker, linopirdine (10 microM), and 82.7 +/- 5.4% (n = 4) by BaCl(2) (10 mM).?The mechanism by which retigabine enhanced KCNQ2/Q3 currents involved large, drug-induced, leftward shifts in the voltage dependence of channel activation (-33.1 +/- 2.6 mV, n = 4, by 10 microM retigabine).?Retigabine shifted the voltage dependence of channel activation with an EC(50) value of 1.6 +/- 0.3 microM (slope factor was 1.2 +/- 0.1, n = 4 to 5 cells per concentration).?Retigabine (0.1 to 10 microM) also slowed the rate of channel deactivation, predominantly by increasing the contribution of a slowly deactivating tail current component.?

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Ezogabine,D-23129

Cell Cycle/DNA Damage

Potassium Channel

KCNQ3/5|KCNQ2/Q3|KCQN4

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150812-13-8

376.25

C16H20Cl2FN3O2

>98% (HPLC)

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Cl.Cl.CCOC(=O)Nc1ccc(NCc2ccc(F)cc2)cc1N

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(-20℃)

With Ice Pack

≥ 2 years