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首页> 外文期刊>Neuropharmacology >Effects of carbamazepine, phenytoin, valproic acid, oxcarbazepine, lamotrigine, topiramate and vinpocetine on the presynaptic Ca(2+) channel-mediated release of ((3)H)glutamate: Comparison with the Na(+) channel-mediated release.
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Effects of carbamazepine, phenytoin, valproic acid, oxcarbazepine, lamotrigine, topiramate and vinpocetine on the presynaptic Ca(2+) channel-mediated release of ((3)H)glutamate: Comparison with the Na(+) channel-mediated release.

机译：卡马西平，苯妥英钠，丙戊酸，奥卡西平，拉莫三嗪，托吡酯和长春西汀对突触前Ca（2+）通道介导的（（3H）H）谷氨酸释放的影响：与Na（+）通道介导的释放的比较。

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The effect of carbamazepine, phenytoin, valproate, oxcarbazepine, lamotrigine and topiramate, that are among the most widely used antiepileptic drugs (AEDs), and of the new putative AED vinpocetine on the Ca(2+) channel-mediated release of [(3)H]Glu evoked by high K(+) in hippocampal isolated nerve endings was investigated. Results show that carbamazepine, oxcarbazepine and phenytoin reduced [(3)H]Glu release to high K(+) to about 30% and 55% at concentrations of 500muM and 1500muM, respectively; lamotrigine and topiramate to about 27% at 1500muM; while valproate failed to modify it. Vinpocetine was the most potent and effective; 50muM vinpocetine practically abolished the high K(+) evoked release of [(3)H]Glu. Comparison of the inhibition exerted by the AEDs on [(3)H]Glu release evoked by high K(+) with the inhibition exerted by the AEDs on [(3)H]Glu release evoked by the Na(+) channel opener, veratridine, shows that all the AEDs are in general more effective blockers of the presynaptic Na(+) than of the presynaptic Ca(2+) channel-mediated response. The high doses of AEDs required to control seizures are frequently accompanied by adverse secondary effects. Therefore, the higher potency and efficacy of vinpocetine to reduce the permeability of presynaptic ionic channels controlling the release of the most important excitatory neurotransmitter in the brain must be advantageous in the treatment of epilepsy.
机译：卡马西平，苯妥英钠，丙戊酸，奥卡西平，拉莫三嗪和托吡酯是最广泛使用的抗癫痫药（AEDs），以及新推定的AED长春西汀对Ca（2+）通道介导的[[（3 ）H] Glu由海马孤立的神经末梢中的高K（+）引起。结果表明，卡马西平，奥卡西平和苯妥英钠分别在500μM和1500μM的浓度下将[（3）H] Glu释放至高K（+）分别降低至约30％和55％。拉莫三嗪和托吡酯在1500μM时约为27％;而丙戊酸盐未能对其进行修改。长春西汀是最有效和有效的。 50μM长春西汀实际上废除了[（3）H] Glu的高K（+）诱发的释放。比较AED对高K（+）引起的[（3）H] Glu释放的抑制作用与AED对Na（+）通道开放剂引起的[（3）H] Glu释放的抑制作用， veratridine，表明所有的AEDs一般比突触前Ca（2+）通道介导的反应更有效地阻滞突触前Na（+）。控制癫痫发作所需的大剂量AED经常伴有不良继发作用。因此，长春西汀降低脑中控制大脑中最重要的兴奋性神经递质释放的突触前离子通道通透性的更高效能和功效在治疗癫痫中必须是有利的。

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