2-甲基-6-苯乙炔基-吡啶（MPEP），一种非竞争性 mGluR5 拮抗剂，对四种传统抗癫痫药物抗杏仁核点燃性癫痫发作的抗惊厥活性有不同的影响。

2-Methyl-6-phenylethynyl-pyridine (MPEP), a non-competitive mGluR5 antagonist, differentially affects the anticonvulsant activity of four conventional antiepileptic drugs against amygdala-kindled seizures in rats.

机构信息

Department of Pathophysiology, Medical University, Jaczewskiego 8, PL 20-090 Lublin, Poland.

出版信息

Pharmacol Rep. 2009 Jul-Aug;61(4):621-30. doi: 10.1016/s1734-1140(09)70114-8.

PMID:19815944

Abstract

2-Methyl-6-phenylethynyl-pyridine (MPEP), a selective noncompetitive mGluR5 antagonist, influences the action of conventional antiepileptic drugs in amygdala-kindled seizures in rats. MPEP alone (up to 40 mg/kg) did not affect any seizure parameter. Moreover, the common treatment of MPEP with either carbamazepine or phenytoin (administered at subeffective doses) did not result in any anticonvulsant action in kindled rats. However, when combined with subprotective doses of valproate or phenobarbital, MPEP significantly shortened seizure and afterdischarge durations. Importantly, combinations of MPEP with the two antiepileptics did not have the adverse effects of impaired motor performance or long-term memory in rats. Our data indicate that MPEP may positively interact with some conventional antiepileptic drugs in the amygdala-kindling model of complex partial seizures.

摘要

2-甲基-6-苯乙炔基-吡啶（MPEP）是一种选择性非竞争性 mGluR5 拮抗剂，可影响杏仁核点燃性癫痫发作大鼠中常规抗癫痫药物的作用。单独使用 MPEP（高达 40mg/kg）不会影响任何癫痫发作参数。此外，用卡马西平或苯妥英（给予亚治疗剂量）常规治疗 MPEP 不会导致点燃大鼠产生抗惊厥作用。然而，当与亚保护剂量的丙戊酸钠或苯巴比妥联合使用时，MPEP 显著缩短了癫痫发作和发作后放电的持续时间。重要的是，MPEP 与这两种抗癫痫药的组合不会对大鼠的运动表现或长期记忆产生不良影响。我们的数据表明，MPEP 可能与杏仁核点燃性部分性癫痫发作模型中的某些常规抗癫痫药物产生积极相互作用。