3-HO-PCP
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| Other names | 3-Hydroxyphencyclidine; 3-OH-PCP; PCP-3-OH |
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3-Hydroxyphencyclidine (3-HO-PCP) is a dissociative of the arylcyclohexylamine class related to phencyclidine (PCP) that has been sold online as a designer drug.[1][2]
Pharmacology
3-HO-PCP acts as a high-
uncompetitive antagonist of the NMDA receptor via the dizocilpine (MK-801) site (Ki = 30 nM).[1][3] It has much higher affinity than PCP for this site (Ki = 250 nM, for comparison; 8-fold difference).[3] The drug also has high affinity for the μ-opioid receptor (MOR) (Ki = 39–60 nM) in animal test subjects,[1][3][4][5] the κ-opioid receptor (KOR) (Ki = 140 nM),[4] and the sigma σ1 receptor (Ki = 42 nM; IC50 = 19 nM),[4][6][7][8] whereas it has only low affinity for the δ-opioid receptor (Ki = 2,300 nM).[4] 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).[3][4]
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.[9][10]
Chemistry
3-HO-PCP is an
dimetamine.[1]
Society and culture
Legal status
On October 18, 2012, the
Misuse of Drugs Act (1971)", despite the fact that the act does not classify drugs based on harm. The report went on to suggest that all analogues of MXE should also become class B drugs and suggested a catch-all clause covering both existing and unresearched arylcyclohexamines, including 3-HO-PCP.[11]
3-HO-PCP is banned in Sweden[12][13] and Switzerland.[14]
See also
References
- ^ PMID 24678061.
- S2CID 216047397.
- ^ PMID 6279847.
- ^ PMID 6088255.
- PMID 6273187.
- PMID 3965930.
- PMID 3036548.
- PMID 2893238.
- PMID 3914938.
- PMID 3724069.
- ^ "(ACMD) Methoxetamine Report (2012)" (PDF). UK Home Office. 2012-10-18. p. 14. Retrieved 2015-06-24.
- ^ "Elva nya ämnen klassas som narkotika eller hälsofarlig vara" [Eleven new substances are classified as narcotics or dangerous goods] (in Swedish). Folkhälsomyndigheten. 28 June 2018.
- ^ "Förordning (1992:1554) om kontroll av narkotika" [Ordinance (1992:1554) on the control of narcotics]. Riksdagsförvaltningen (in Swedish).
- ^ "Verordnung des EDI vom 30. Mai 2011 über die Verzeichnisse der Betäubungsmittel, psychotropen Stoffe, Vorläuferstoffe und Hilfschemikalien (Betäubungsmittelverzeichnisverordnung, BetmVV-EDI)" [EDI ordinance of May 30, 2011 on the lists of narcotics, psychotropic substances, precursors and auxiliary chemicals (narcotics list ordinance, BetmVV-EDI)] (in German). Der Bundesrat.