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右美沙芬:减轻神经元过度活跃的细胞效应。

Dextromethorphan: cellular effects reducing neuronal hyperactivity.

作者信息

Trube G, Netzer R

机构信息

Pharma Division, F. Hoffmann-La Roche Ltd., Basel, Switzerland.

出版信息

Epilepsia. 1994;35 Suppl 5:S62-7. doi: 10.1111/j.1528-1157.1994.tb05972.x.

DOI:10.1111/j.1528-1157.1994.tb05972.x
PMID:7518769
Abstract

Dextromethorphan is a dextrorotary morphinan without affinity for opioid receptors, commonly used as an antitussive medication. During the past 5 years, interest in the compound and its demethylated derivative, dextrorphan, has been revived because additional neuroprotective and antiepileptic properties were found in in vitro studies, animal experiments, and a few clinical cases. Both morphinans are able to inhibit N-methyl-D-aspartate (NMDA) receptor channels and voltage-operated calcium and sodium channels with different potencies. The inhibition of the NMDA receptor is believed to be the predominant mechanism of action responsible for the anticonvulsant and neuroprotective properties of the compounds.

摘要

右美沙芬是一种对阿片受体无亲和力的右旋吗啡喃,常用作镇咳药。在过去5年中,人们对该化合物及其去甲基衍生物右啡烷的兴趣再度兴起,因为在体外研究、动物实验和一些临床病例中发现了它们额外的神经保护和抗癫痫特性。这两种吗啡喃都能够以不同的效力抑制N-甲基-D-天冬氨酸(NMDA)受体通道以及电压门控钙通道和钠通道。对NMDA受体的抑制被认为是这些化合物具有抗惊厥和神经保护特性的主要作用机制。

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Dextromethorphan: cellular effects reducing neuronal hyperactivity.右美沙芬:减轻神经元过度活跃的细胞效应。
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Dextromethorphan blocks N-methyl-D-aspartate-induced currents and voltage-operated inward currents in cultured cortical neurons.右美沙芬可阻断培养的皮质神经元中N-甲基-D-天冬氨酸诱导的电流和电压依赖性内向电流。
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Binding of dimemorfan to sigma-1 receptor and its anticonvulsant and locomotor effects in mice, compared with dextromethorphan and dextrorphan.与右美沙芬和右啡烷相比,二甲吗啡对小鼠σ-1受体的亲和力及其抗惊厥和运动效应。
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