抗癫痫药物、钙通道阻滞剂及其他化合物对DBA/2小鼠电压依赖性L型钙通道激活所致癫痫发作的影响。

Effects of antiepileptic drugs, calcium channel blockers and other compounds on seizures induced by activation of voltage-dependent L calcium channel in DBA/2 mice.

De Sarro G, Ascioti C, di Paola E D, Vidal M J, De Sarro A

Institute of Pharmacology, Faculty of Medicine and Surgery, University of Reggio Calabria, Italy.

Gen Pharmacol. 1992 Nov;23(6):1205-16. doi: 10.1016/0306-3623(92)90313-9.

Abstract

The convulsant activity of the calcium voltage L-channel agonist Bay k 8644 was studied in genetically epilepsy prone DBA/2 mice. 2. Seizures were induced by intracerebroventricular injection of Bay k 8644. 3. These seizures were reversed by some calcium channel blockers such as dihydropyridines, some excitatory amino acid antagonists such as 2-amino-7-phosphonoeptanoate and CPPene, 2-chloro-adenosine, some anticonvulsant drugs such as magnesium valproate, diazepam and clonazepam and two kappa opioid agonists (U-50488H and U-54494A). 4. The remaining antiepileptic drugs (carbamazepine, phenytoin, phenobarbital and trimethadione) were ineffective in this respect. Other anticonvulsant compounds such as dizocilpine (MK 801), ketamine and drugs enhancing GABAergic transmission did not significantly affect the clonic phase of the seizures induced by Bay k 8644. 5. These results show that Bay k 8644 seizures are relatively resistant to some anticonvulsant compounds. The role of some neurotransmitters on seizures induced by Bay k 8644 is discussed.

摘要

在遗传性癫痫易感的DBA/2小鼠中研究了钙电压L通道激动剂Bay k 8644的惊厥活性。2. 通过脑室内注射Bay k 8644诱发癫痫发作。3. 这些癫痫发作可被一些钙通道阻滞剂（如二氢吡啶类）、一些兴奋性氨基酸拮抗剂（如2-氨基-7-膦酰庚酸和CPPene）、2-氯腺苷、一些抗惊厥药物（如丙戊酸镁、地西泮和氯硝西泮）以及两种κ阿片受体激动剂（U-50488H和U-54494A）逆转。4. 其余的抗癫痫药物（卡马西平、苯妥英、苯巴比妥和三甲双酮）在这方面无效。其他抗惊厥化合物，如地佐环平（MK 801）、氯胺酮以及增强GABA能传递的药物，对Bay k 8644诱发的癫痫发作的阵挛期没有显著影响。5. 这些结果表明，Bay k 8644诱发的癫痫发作对一些抗惊厥化合物具有相对抗性。讨论了一些神经递质在Bay k 8644诱发的癫痫发作中的作用。