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托吡酯:杏仁核点燃大鼠中的一种强效抗惊厥药。

Topiramate: a potent anticonvulsant in the amygdala-kindled rat.

作者信息

Wauquier A, Zhou S

机构信息

Department of Neurology, Texas Tech University Health Sciences Center, Lubbock 79430, USA.

出版信息

Epilepsy Res. 1996 Jun;24(2):73-7. doi: 10.1016/0920-1211(95)00105-0.

Abstract

Topiramate, a chemically novel anti-epileptic drug, was evaluated in amygdala-kindled seizures in rats. Topiramate, given at doses between 0.63 and 80 mg/kg i.p. and p.o. 4 h before kindling stimulation, exhibited a dose-related inhibition on all seizure parameters measured, i.e. behavioral seizures, forelimb clonus, amygdala and cortical afterdischarges. The ED50 values obtained with topiramate on kindled seizures in all parameters tended to be lower than those observed on maximal electroshock seizures in rats. After oral drug administration, the ED50 values were: on forelimb clonus, 7.25 mg/kg; on amygdala afterdischarges 7.09 mg/kg and on cortical afterdischarges 7.12 mg/kg. After i.p. drug administration, the ED50 values were: on forelimb clonus, 10.6 mg/kg; on amygdala afterdischarges, 13.9 mg/kg and on cortical afterdischarges, 10.4 mg/kg. The data obtained after i.p. drug administration are in line with the suggestion that topiramate primarily blocks spread of seizures.

摘要

托吡酯是一种化学结构新颖的抗癫痫药物,在大鼠杏仁核点燃性癫痫发作模型中进行了评估。在点燃刺激前4小时腹腔注射和口服给予托吡酯,剂量范围为0.63至80mg/kg,对所测量的所有癫痫发作参数均呈现出剂量依赖性抑制,即行为性癫痫发作、前肢阵挛、杏仁核和皮层后放电。托吡酯在所有参数上对点燃性癫痫发作的半数有效剂量(ED50)值往往低于在大鼠最大电休克癫痫发作中观察到的值。口服给药后,ED50值分别为:前肢阵挛7.25mg/kg;杏仁核后放电7.09mg/kg;皮层后放电7.12mg/kg。腹腔注射给药后,ED50值分别为:前肢阵挛10.6mg/kg;杏仁核后放电13.9mg/kg;皮层后放电10.4mg/kg。腹腔注射给药后获得的数据符合托吡酯主要阻断癫痫发作传播的观点。

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