Influence of calcium channel blockers on pentylenetetrazol and electroshock-induced convulsions in mice.

E Jagiełło-Wójtowicz, S J Czuczwar, A Chodkowska, J Szponar, Z Kleinrok
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Abstract

Nifedipine (2.5-10 mg/kg) and verapamil (2.5 and 10 mg/kg) offered some protection against pentylenetetrazol (100 and 130 mg/kg)-induced seizure activity in mice. No protection was provided by diltiazem (1.25-10 mg/kg) in this model of experimental epilepsy. Repeated administration of calcium channel blockers (CCBs) in doses of 5 and 10 mg/kg twice daily for three days resulted in no protective effect against pentylenetetrazol. Regarding electroconvulsions, nifedipine (2.5-10 mg/kg) showed the best anticonvulsive action--for instance, in the dose of 10 mg/kg (60 min--treatment time) it elevated the threshold for electroconvulsions from 7.1 to 10.5 mA. Diltiazem (up to 10 mg/kg) and verapamil (up to 20 mg/kg) were considerably less potent in this respect. After repeated administration, only nifedipine (5-10 mg/kg) retained its protective action against electroconvulsions.

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钙通道阻滞剂对戊四氮和电休克小鼠惊厥的影响。
硝苯地平(2.5-10 mg/kg)和维拉帕米(2.5和10 mg/kg)对戊四氮(100和130 mg/kg)引起的小鼠癫痫发作活动有一定的保护作用。地尔硫卓(1.25 ~ 10 mg/kg)对该实验性癫痫模型无保护作用。反复服用钙通道阻滞剂(CCBs),剂量分别为5和10mg /kg,每天两次,连续3天,对戊四氮没有保护作用。对于电惊厥,硝苯地平(2.5-10 mg/kg)表现出最好的抗惊厥作用——例如,在10 mg/kg(60分钟治疗时间)的剂量下,它将电惊厥的阈值从7.1 mA提高到10.5 mA。地尔硫卓(高达10毫克/公斤)和维拉帕米(高达20毫克/公斤)在这方面的效力要低得多。反复给药后,只有硝苯地平(5-10 mg/kg)保留其对电惊厥的保护作用。
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