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Encyclopedia > Dextrorphan

Dextrorphan is a pharmacologically active metabolite of Dextromethorphan (DXM). It is the result of O-demethylation of the prodrug by several enzymatic systems, although it is chiefly a product of the Cytochrome P450 IID6 (CYP4502D6) pathway. Being structurally similar to DXM, and it has affinity for the same receptors in the central nervous system but with a slight difference in selectivity. Whereas DXM has the highest binding-affinity for PCP2 and sigma receptors, DXO is more selective for NMDA receptors. DXO is a strong anti-tussive, but is slightly less effective than DXM, and has no metabolites with significant therapeutic activity in such capacity and therefore is not a drug available on the market. A prodrug is a pharmacological substance (drug) which is administered in an inactive (or significantly less active) form. ... The Central Nervous System (CNS) represents the largest part of the Nervous System. ...


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UGA Physiology and Pharmacology | Faculty and Research | Thomas F. Murray (244 words)
In the area of drug abuse research we are utilizing dextrorphan as a novel radioligand probe for phencyclidine (PCP) receptors.
Dextrorphan shares with PCP and ketamine the ability to act as a non-competitive antagonist of N-methyl-D-aspartate (NMDA) receptors in the central nervous system.
Notwithstanding the commonalities of action of dextrorphan and PCP, the mechanism of dextrorphan interaction with the ion channel domain in the NMDA receptor appears distinctive.
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