3-Hydroxymorphinan

3-Hydroxymorphinan is an active metabolite of the opioid analgesic drug dextromethorphan. It is formed in the body after the administration of dextromethorphan and is responsible for some of the drug's analgesic effects.

Pharmacology

3-Hydroxymorphinan acts as an antagonist at the NMDA receptor, which is a type of glutamate receptor that plays a key role in learning and memory. By blocking this receptor, 3-Hydroxymorphinan can reduce the perception of pain.

In addition to its NMDA receptor antagonism, 3-Hydroxymorphinan also has affinity for the sigma-1 receptor, which is involved in the regulation of neurotransmitter release. This may contribute to its analgesic effects.

Clinical Use

3-Hydroxymorphinan is not used clinically on its own, but is formed in the body after the administration of dextromethorphan. Dextromethorphan is used as a cough suppressant and also has analgesic properties. The formation of 3-Hydroxymorphinan contributes to these analgesic effects.

Side Effects

As a metabolite of dextromethorphan, 3-Hydroxymorphinan can contribute to the side effects of this drug. These can include nausea, vomiting, dizziness, and sedation. In rare cases, high doses of dextromethorphan can lead to a serious condition called serotonin syndrome, which is characterized by agitation, hallucinations, rapid heartbeat, and high body temperature.

See Also

• Dextromethorphan
• NMDA receptor antagonist
• Sigma-1 receptor