3-Methyl-PCPy (3-Me-PCPy) is an arylcyclohexylamine derivative with an unusual spectrum of pharmacological effects, acting as both a potent NMDA antagonist and also a triple reuptake inhibitor which inhibits reuptake of all three monoamine neurotransmitters serotonin, dopamine and noradrenaline. It also acts as a high affinity sigma receptor ligand, selective for the σ2 subtype. It produces both stimulant and dissociative effects in animal behavioural studies.
Pharmacology In in vitro binding assays, 3-Me-PCPy displays high affinities across monoamine reuptake transporters alongside the NMDA receptor complex. Unusually for an arylcyclohexylamine dissociative, its affinity for the serotonin transporter (SERT) is approximately ten-fold higher than its affinity for the NMDA receptor pore.
+ Binding affinities of 3-Me-PCPy (Wallach & Brandt, 2018) Target site Assay / Site Ki (nM) Serotonin transporter (SERT) Monoamine reuptake 5.6 Dopamine transporter (DAT) Monoamine reuptake 39.0 Norepinephrine transporter (NET) Monoamine reuptake 45.0 NMDA receptor Dizocilpine (MK-801) site 52.3
Legal Status 3-Methyl-PCPy is covered by drug analogue laws in various jurisdictions (UK, Germany, Japan, Australia etc.) as a generic arylcyclohexylamine derivative, and a structural isomer of phencyclidine.
See also 3-Methyl-PCP 3-HO-PCE BTCP Deoxymethoxetamine Ephenidine MDPCP
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