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Properties of human brain sodium channel α-subunits expressed in HEK293 cells and their modulation by carbamazepine phenytoin and lamotrigine

机译:人脑钠通道α亚基在HEK293细胞中表达的特性及其对卡马西平苯妥英钠和拉莫三嗪的调节作用

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摘要

Background and purposeVoltage-activated Na+ channels contain one distinct α-subunit. In the brain NaV1.1, NaV1.2, NaV1.3 and NaV1.6 are the four most abundantly expressed α-subunits. The antiepileptic drugs (AEDs) carbamazepine, phenytoin and lamotrigine have voltage-gated Na+ channels as their primary therapeutic targets. This study provides a systematic comparison of the biophysical properties of these four α-subunits and characterizes their interaction with carbamazepine, phenytoin and lamotrigine.
机译:背景和目的电压激活的Na + 通道包含一个不同的α-亚基。在大脑中,NaV1.1,NaV1.2,NaV1.3和NaV1.6是四个表达最丰富的α亚基。抗癫痫药卡马西平,苯妥英钠和拉莫三嗪以电压门控的Na + 通道为主要治疗靶点。该研究提供了这四个α-亚基的生物物理特性的系统比较,并表征了它们与卡马西平,苯妥英钠和拉莫三嗪的相互作用。

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