Wong B Y, Coulter D A, Choi D W, Prince D A
Department of Neurology, Stanford University, CA 94305.
Neurosci Lett. 1988 Feb 29;85(2):261-6. doi: 10.1016/0304-3940(88)90362-x.
The antitussive, dextromethorphan (DM), and its metabolite, dextrorphan (DX), were evaluated for antiepileptic properties in vitro. Interictal bursts and prolonged ictal epileptiform afterdischarges, induced by perfusion of guinea pig neocortical brain slices with Mg2+-free solution, were blocked by DX (1-250 microM) or DM (100 microM). Intracellular records showed that these agents blocked N-methyl-D-aspartate (NMDA)-induced depolarizations without altering intrinsic membrane properties. DX blocked NMDA but not quisqualate-evoked multi-unit excitatory responses. DM is a widely available, orally effective drug with low toxicity in antitussive doses, which has antiepileptic and NMDA-antagonist properties in vitro. Its toxicity and effectiveness as an anticonvulsant should be expeditiously examined in clinical trials.
对镇咳药右美沙芬（DM）及其代谢产物右啡烷（DX）进行了体外抗癫痫特性评估。用无镁溶液灌注豚鼠新皮质脑片所诱发的发作间期爆发和延长的发作期癫痫样后放电，被DX（1 - 250微摩尔）或DM（100微摩尔）阻断。细胞内记录显示，这些药物可阻断N - 甲基 - D - 天冬氨酸（NMDA）诱导的去极化，而不改变固有膜特性。DX阻断NMDA诱发的反应，但不阻断 quisqualate诱发的多单位兴奋性反应。DM是一种广泛可得的口服有效药物，在镇咳剂量下毒性较低，在体外具有抗癫痫和NMDA拮抗剂特性。应在临床试验中迅速检查其作为抗惊厥药的毒性和有效性。
