Dextrallorphan
chemical compound
Dextrallorphan (DXA) is a chemical of the morphinan class that is used in scientific research. It acts as a σ1 receptor agonist and NMDA receptor antagonist. It has no significant affinity for the σ2, μ-opioid, or δ-opioid receptor, or for the serotonin or norepinephrine transporter.
As an NMDA receptor antagonist, in vivo, it is approximately twice as potent as dextromethorphan, and five-fold less potent than dextrorphan.
Uses in Scientific Research
Masking of sigma-1 receptor
Dextrallorphan is often used in research to block σ1 receptor sites so that σ2 receptor sites (which have not been cloned yet ) can be studied.
It was hypothesized that both of these sigma (σ) receptors were opioid receptors, due to their affinity for psychoactive drugs. However, it is now understood that they are non-opioid receptors that bind to certain psychoactive drugs, like dextrallorphan.
One example of dextrallorphan being used to mask σ1 receptor sites was seen in a study on the localization of the σ2 receptor in detergent-resistant lipid raft domains. It has also been used to mask σ1 receptor sites so that σ2 receptor binding characteristics in the rat liver could be determined, by labeling σ2 receptor sites with [3H]l,3-di-o-tolylguanidine (DTG) in the presence of 1 μM dextrallorphan solution.
Animal Studies
Dextrallorphan was used in Spraque-Dawley rats to study cerebellar Purkinje neurons electrophysical responses to the drug when it was applied iontophoretically as a sigma (σ) receptor ligand.
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