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钙通道阻滞剂对大鼠实验性诱导癫痫发作的影响。

Effect of calcium channel blockers on experimentally induced seizures in rats.

作者信息

Kamal J A, Nadig R S, Joseph T, David J

机构信息

Department of Pharmacology, St. John's Medical College, Bangalore, India.

出版信息

Indian J Exp Biol. 1990 Jul;28(7):605-8.

PMID:2272645
Abstract

Chemically different classes of calcium channel blockers were examined in rats for their effects on behavior, tolerability and protection against maximal electroshock seizures (MES) and pentylenetetrazol (PTZ) induced seizures. In MES test at doses (mg/kg, ip) that were devoid of side effects, felodipine, 50, afforded 100% protection, while nimodipine, 5; pimozide, 10; and thioridazine, 25, showed 50 to 66% protection. Nifedipine, 10, and diltiazem, 50, showed 30 and 66% protection respectively, but were associated with side effects. Verapamil and loperamide were ineffective against MES and PTZ induced seizures. Nimodipine, 1 mg/kg, ip, was the most potent agent and produced 100% protection against PTZ. Equieffective doses were pimozide, 25, felodipine, 50, and thioridazine, 50. The rest of the calcium channel blockers showed marginal to moderate activity against chemoshock. The data obtained suggest that some calcium channel blockers possess anticonvulsant activity and may be considered as adjuvant therapeutic agents in epileptics refractory to conventional antiepileptic medication.

摘要

在大鼠中研究了化学性质不同的几类钙通道阻滞剂对行为、耐受性以及对最大电休克惊厥(MES)和戊四氮(PTZ)诱导惊厥的保护作用。在MES试验中,在无副作用的剂量(mg/kg,腹腔注射)下,非洛地平50mg/kg可提供100%的保护,而尼莫地平5mg/kg、匹莫齐特10mg/kg和硫利达嗪25mg/kg的保护率为50%至66%。硝苯地平10mg/kg和地尔硫䓬50mg/kg的保护率分别为30%和66%,但伴有副作用。维拉帕米和洛哌丁胺对MES和PTZ诱导的惊厥无效。尼莫地平1mg/kg腹腔注射是最有效的药物,对PTZ诱导的惊厥产生100%的保护作用。等效剂量的有匹莫齐特25mg/kg、非洛地平50mg/kg和硫利达嗪50mg/kg。其余的钙通道阻滞剂对化学性休克表现出轻微至中等程度的活性。获得的数据表明,一些钙通道阻滞剂具有抗惊厥活性,可被视为常规抗癫痫药物治疗无效的癫痫患者的辅助治疗药物。

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