Description
Dextromethorphan (DXM) is a dextratrorotatory morphinan with structural similarity to levorphanol, codeine, and morphine. Because of its strong antitussive effects, dextromethorphan is widely used as a cough suppressant. However, it does not provoke opioid activity as is characteristic of several other morphine derivatives. DXM binds to and inhibits NMDA (IC
50 = 0.55 μM) and nicotinic receptors (IC
50s = 0.7-
3.9 μM) and blocks receptor-
gated and voltage-
gated calcium channels (IC
50 = 60 μM) and voltage-
gated sodium channels (IC
50 = 78 μM). DXM has been used in multimodal analgesic therapies for acute and neuropathic pain.
Biological Activity
Non-competitive, low affinity NMDA receptor antagonist. Antitussive, anticonvulsive and neuroprotective agent.