Retigabine dihydrochloride 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。作用机制涉及神经元 K(V)7.2-7.5（以前的 KCNQ2-5）电压激活 K(+) 通道的开放。

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[1].

150812-13-8

C16H20Cl2FN3O2

376.25

D-23129;瑞替加滨;Ezogabine;Retigabine dihydrochloride

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years