3-HO-PCP also known as: 3-Hydroxyphencyclidine is a dissociative of the Arylcyclohexylamine class related to Phencyclidine (PCP)

3-HO-PCP acts as a high-affinity uncompetitive antagonist of the NMDA receptor via the dizocilpine (MK-801) site (Ki = 30 nM).

It has much higher affinity than PCP for this site (Ki = 250 nM, for comparison; 8-fold difference).

The drug also has high affinity for the μ-opioid receptor (MOR) (Ki = 39–60 nM) in animal test subjects, the κ-opioid receptor (KOR) (Ki = 140 nM), and the sigma σ1 receptor (Ki = 42 nM; IC50 = 19 nM), whereas it has only low affinity for the δ-opioid receptor (Ki = 2,300 nM).

The high affinity of 3-HO-PCP for opioid receptors is unique among arylcyclohexylamines and is in contrast to PCP, which has only very low affinity for the MOR (Ki = 11,000–26,000 nM; 282- to 433-fold difference) and the other opioid receptors (Ki = 4,100 nM for the KOR and 73,000 nM for the DOR).

Although it was hypothesized that 3-HO-PCP might be a metabolite of PCP in humans, there is no evidence that this is the case.

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