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调节神经元谷氨酸摄取的钠通量:局部麻醉药和抗惊厥药的不同作用

Sodium fluxes modulating neuronal glutamate uptake: differential effects of local anesthetic and anticonvulsant drugs.

作者信息

Taylor C A, Tsai C, Lehmann J

机构信息

Ciba-Geigy Corporation, Pharmaceuticals Division, Summit, New Jersey.

出版信息

J Pharmacol Exp Ther. 1988 Feb;244(2):666-73.

PMID:2450198
Abstract

Local anesthetics and anticonvulsant drugs were differentiated biochemically by quantitating their effects on aconitine- and ouabain-induced inhibition of L-[3H]glutamate uptake in synaptosomes. Amine local anesthetics reversed the inhibition by both compounds whereas the anticonvulsant drugs such as carbamazepine and diphenylhydantoin reversed the effects of aconitine but not ouabain. These results support the concept that carbamazepine and diphenylhydantoin interact with voltage-sensitive Na channels to block Na conductance whereas the amine local anesthetics are less specific in their actions.

摘要

通过定量分析局部麻醉药和抗惊厥药对乌头碱和哇巴因诱导的突触体中L-[3H]谷氨酸摄取抑制作用的影响,对它们进行了生化区分。胺类局部麻醉药可逆转这两种化合物的抑制作用,而卡马西平和苯妥英等抗惊厥药可逆转乌头碱的作用,但不能逆转哇巴因的作用。这些结果支持了这样一种观点,即卡马西平和苯妥英与电压敏感性钠通道相互作用以阻断钠电导,而胺类局部麻醉药的作用则缺乏特异性。

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