3-MeO-PCP

Pharmacology

3-MeO-PCP has a K_i of 20 nM for the dizocilpine (MK-801) site of the NMDA receptor, 216 nM for the serotonin transporter (SERT), and 42 nM for the sigma σ₁ receptor. It does not bind to the norepinephrine or dopamine transporter nor to the sigma σ₂ receptor (K_i >10,000 nM). Based on its structural similarity to 3-hydroxy-PCP (3-HO-PCP), which uniquely among arylcyclohexylamines has high affinity for the μ-opioid receptor in addition to the NMDA receptor, it was initially expected that 3-MeO-PCP would have opioid activity. However, radioligand binding assays with human proteins have shown that, contrary to common belief, the drug also does not interact with the μ-, δ-, or κ-opioid receptors at concentrations of up to 10,000 nM. As such, the notion that 3-MeO-PCP has opioid activity has been described as a myth.