Methoxetamine: from drug of abuse to rapid-acting antidepressant.

Methoxetamine, a dissociative anesthetic similar to ketamine, may produce rapid antidepressant effects in patients with resistant and non-resistant unipolar and bipolar depression. Like ketamine, it acts as a noncompetitive NMDA receptor antagonist and dopamine reuptake inhibitor, and also binds to dopamine D2, serotonin 5HT2, muscarinic cholinergic, sigma-1, and opioid mu and k receptors. The hypothesis is that these pharmacodynamic properties could lead to rapid mood improvement, but no empirical results are reported.

Study at a glance

Abstract

Methoxetamine is a dissociative anaesthetic showing pharmacodynamic similarities with its analogue ketamine, a medication with demonstrated rapid-acting antidepressant effects. Like ketamine and other arylcyclohexylamine compounds, methoxetamine is thought to be both a noncompetitive NMDA receptor antagonist and a dopamine reuptake inhibitor. Furthermore, it acts as an agonist at dopamine D2, serotonin 5HT2, muscarinic cholinergic, sigma-1, opioid mu and k receptors. The hypothesis is that methoxetamine can produce rapid antidepressant effects in patients with resistant and non-resistant unipolar and bipolar depression.