Dextromethorphan: cellular effects reducing neuronal hyperactivity.
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.
Trube
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Pharma Division, F. Hoffmann-La Roche Ltd., Basel, Switzerland.
Netzer
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D000818:Animals; D015220:Calcium Channels / Q000187:drug effects / Q000502:physiology; D002478:Cells, Cultured; D003915:Dextromethorphan / Q000494:pharmacology* / Q000627:therapeutic use; D003917:Dextrorphan / Q000494:pharmacology / Q000627:therapeutic use; D004594:Electrophysiology; D005071:Evoked Potentials / Q000187:drug effects; D006801:Humans; D007473:Ion Channels / Q000187:drug effects* / Q000502:physiology; D009474:Neurons / Q000187:drug effects; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate / Q000187:drug effects; D012640:Seizures / Q000517:prevention & control; D015222:Sodium Channels / Q000187:drug effects / Q000502:physiology
D015220:Calcium Channels; D007473:Ion Channels; D016194:Receptors, N-Methyl-D-Aspartate; D015222:Sodium Channels; D003917:Dextrorphan; D003915:Dextromethorphan