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Retigabine

瑞替加濱

Mechanism of action:

Retigabine 是一種電壓門控鉀離子通道開啟劑(voltage-gated potassium channel opener)。Retigabine 直接作用於 KCNQ2、KCNQ3 鉀離子通道,這些通道負責產生 M 電流(M-current),是控制神經元靜息電位(resting potential)與動作電位閾值(action potential threshold)的重要電流。Retigabine 會使這些鉀離子通道的活化電位向過極化方向位移,讓鉀離子外流增加,細胞膜超極化(hyperpolarization),抑制動作電位的重複放電。

​Reference(s):

1. Porter RJ et al. (2007). Retigabine. Neurotherapeutics. 


2. Hermann R et al. (2003). Effects of age and sex on the disposition of retigabine. Clin Pharmacol Ther. 


3. Hermann R et al. (2003). Pharmacokinetic interaction between retigabine and lamotrigine in healthy subjects. Eur J Clin Pharmacol.

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