3-HO-PCP

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Summary sheet: 3-HO-PCP
3-HO-PCP
Molecular structure of 3-HO-PCP
3-HO-PCP.svg
Chemical Nomenclature
Common names 3-HO-PCP, Hydroxyphencyclidine
Substitutive name 3-Hydroxyphencyclidine
Systematic name 3-(1-Piperidin-1-ylcyclohexyl)phenol
Class Membership
Psychoactive class Dissociative / Opioid
Chemical class Arylcyclohexylamine
Routes of Administration

WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.



Oral
Dosage
Threshold mg
Light 2 - 4 mg
Common 4 - 6 mg
Strong 6 - 8 mg
Heavy 8 mg + Redosing may result in dangerous cumulative effects.
Duration
Total 4 - 6 hours
Come up 60 - 90 minutes









DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.

3-Hydroxyphencyclidine (commonly known as 3-HO-PCP) is a novel synthetic dissociative substance of the arylcyclohexylamine chemical class that produces potent, highly dose-sensitive dissociative, hallucinogenic and euphoric effects when administered. In addition to its primary activity as a NMDA receptor antagonist, it has been found to have appreciable affinity for the μ-opioid receptor.[1]

3-HO-PCP was first synthesized in 1978 to investigate the structure-activity relationship of phencyclidine (PCP) derivatives.[2] It was further explored alongside PCP in the 1980s, where it was discovered to possess μ-opioid agonist activity in animal models.[1]

Like other substances of its class, particularly methoxetamine (MXE), phencyclidine (PCP), and 3-MeO-PCE, it is known to primarily induce a state referred to as "dissociative anesthesia", albeit the extent to which this occurs has been reported to be highly dose-dependent and variable in its effects.[citation needed] It is unknown whether the studied opioid properties in animal models applies to humans, with some early reports suggesting that it does not.

There are also reports that suggest this compound may produce more physical side effects such as muscle soreness and flu-like symptoms during or shortly after administration. This suggests it may be uniquely more dangerous or toxic than related dissociatives, particularly at higher doses.

Today, 3-HO-PCP is almost exclusively distributed as a gray area research chemical by online vendors.[3] Extremely little is known about its pharmacology, metabolism and toxicity in humans. Due to its sensitive dose-response, potential habit-forming properties, as well as unknown toxicity profile, it is strongly recommended that one use proper harm reduction practices if choosing to use this substance.

History and culture

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3-HO-PCP was first synthesized in 1978 to investigate the structure-activity relationship of phencyclidine (PCP) derivatives.[2] It was further explored alongside PCP in the 1980s, where it was discovered to possess μ-opioid agonist activity in animal models.[1]

Its potential as a research chemical for human use was not suggested until 1999 when a chemist using the pseudonym John Q. Beagle reported on its significantly increased potency relative to PCP as well as its "profoundly enhanced affinity for the opiate receptor" which was estimated to give it analgesic activity one order of magnitude lower than morphine.[4][5]

On October 18, 2012, the Advisory Council on the Misuse of Drugs in the United Kingdom released a report about methoxetamine, saying that the "harms of methoxetamine are commensurate with Class B of the Misuse of Drugs Act (1971)", despite the fact that the act does not classify drugs based on harm. The report suggests that all analogs of MXE should also become class B drugs and suggested a catch-all clause covering both existing and unresearched arylcyclohexamines, including 3-HO-PCP.[6]

Chemistry

3-HO-PCP, or 3-hydroxyphencyclidine, is a synthetic dissociative of the arylcyclohexylamine class. The structure of 3-HO-PCP is comprised of cyclohexane, a six-member saturated ring, bonded to two additional rings at R1. One of these rings is a piperidine ring, a nitrogenous six member ring, bonded at its nitrogen group. The other ring is an aromatic phenyl ring, substituted at R3 with a hydroxy group.

3-HO-PCP is a structural analog of PCP and a homolog 3-MeO-PCP.

Pharmacology

Further information: NMDA receptor antagonist

Like other arylcyclohexylamine dissociatives, 3-HO-PCP acts principally as an NMDA receptor antagonist.[2]

The NMDA (N-Methyl-D-Aspartate) receptor, a specific subtype of the glutamate receptor, modulates the transmission of electrical signals between neurons in the brain and spinal cord; for the signals to pass, the receptor must be open. Dissociatives inhibit the normal functioning NMDA receptors by binding to and blocking them. This disruption of neural network activity causes network disintegration, some research suggests, by hyperconnectivity throughout the brain. This causes an increase in noise (random, nonsensical and erraneous data) on the cerebral network and thus produces loss of normal cognitive and affective processing, psychomotor functioning, anesthesia. This is often observed in those showing psychosis or induced with high-dose IV THC or ketamine in healthy participants, please see references. [7][8][9]

Unlike many other dissociatives, 3-HO-PCP has also been found to have appreciable affinity as a μ-opioid receptor agonist in animal models.[1] However, the extent to which this applies to humans remains unknown.

Subjective effects

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The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances and are more likely to induce a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include injury or death.

Physical effects
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Disconnective effects
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Experience reports

Anecdotal reports which describe the effects of this compound within our experience index include:


Toxicity and harm potential

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We also recommend that you practice diligent independent research and the most thorough harm reduction practices when using this substance.

The toxicity and long-term health effects of recreational 3-HO-PCP use have not been studied in any scientific context and the exact toxic dosage is unknown. This is because 3-HO-PCP has an extremely brief history of human usage.

Tolerance and addiction potential

While evidence is lacking, early reports suggest that the chronic use of 3-HO-PCP is likely to be moderately addictive with a high potential for adverse side effects such as psychosis. As with the closely related analog 3-MeO-PCP, reports suggest that 3-HO-PCP may be more habit-forming than dissociatives such as MXE, diphenidine, ephenidine, DCK, and ketamine. When addiction has developed, cravings and withdrawal effects may occur if a person suddenly stops their usage.

Tolerance to many of the effects of 3-HO-PCP is thought to develop with prolonged and repeated use. If true, this would require users to administer increasingly large doses to achieve the same effects. After that, it likely takes about 4 - 7 days for the tolerance to be reduced to half and 1 - 2 weeks to be back at baseline (in the absence of further consumption). 3-HO-PCP likely presents cross-tolerance with all dissociatives, meaning that after the use of 3-HO-PCP, all dissociatives will have a reduced effect.

It is recommended that one exercise extreme caution and harm reduction practices when using this substance.

  • Users should avoid taking the substance multiple days in a row or becoming dependent/addicted to it as this seems to be the main common factor in the observed incidences of severe adverse effects associated with closely related substances like 3-MeO-PCP.
  • The recommended dosage range should not be exceeded as high doses are likely to trigger these effects as well.
  • Users should start with extremely low doses and work their way up as slowly as possible. Volumetric liquid dosing should preferably be used due to the drug's potency; most standard milligram scales cannot accurately weigh out doses below 10-15mg.[10]
  • Compulsive redosing before one has fully sobered up is not recommended and can result in too high of a dose being administered, which may result in highly unpredictable side effects.

Due to the potential risk of psychosis, it is not recommended to combine 3-HO-PCP with any other substances, especially stimulants, psychedelics, or other dissociatives. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.

It is strongly recommended that one use harm reduction practices, such as volumetric dosing, when using this substance to ensure the administration of the intended dose.

Urinary tract effects

3-HO-PCP is likely to exhibit similar bladder and urinary tract problems to those found within ketamine when used repeatedly and excessively for extended periods of time, but to a lesser extent. This is likely because 3-HO-PCP is far more potent than ketamine, so significantly less of drug needs to be consumed. Symptoms of ketamine-induced cystitis can become extremely serious and can be described as:

  • Urinary frequency - Urinary frequency is the need to empty the bladder every few minutes.
  • Urinary urgency - This can be described as a sudden, compelling need to urinate.
  • Urinary pressure - This is experienced as a constant sensation of fullness in the bladder that is unrelieved by urination.
  • Pelvic and bladder pain - Pain can develop suddenly and severely, particularly as the bladder fills with urine.
  • Hematuria - Hematuria is visible blood in the urine.
  • Incontinence - This is the leakage of urine.

Dangerous interactions

Prominent examples include PCP and its analogs 3-MeO-PCP, MXE, and the diarylethylamine dissociatives like diphenidine or ephenidine. There is also evidence that suggests that combining these two increases their neurotoxicity.[citation needed] Anecdotally, worsened comedowns are also commonly reported when these two classes of substances are combined.
  • Depressants - Because both depress the respiratory system, this combination can result in an increased risk of suddenly falling unconscious, vomiting and choking to death from the resulting suffocation. If nausea or vomiting occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.

Legality

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  • United Kingdom - 3-HO-PCP is a class B drug in the UK and is illegal to possess, produce, supply, or import. As a derivative of 1-Phenylcyclohexylamine where the amine has been replaced with a 1-piperidyl group, further substituted in the phenyl ring with a hydroxy substituent, it is covered by the arylcyclohexylamine generic clause added to the Misuse of Drugs Act by S.I. 2013/239, which came into effect on the 26th February 2013.[11]

See also

External links

Literature

  • Morris, H., & Wallach, J. (2014). From PCP to MXE: A comprehensive review of the non-medical use of dissociative drugs. Drug Testing and Analysis, 6(7–8), 614–632. https://doi.org/10.1002/dta.1620
  • Kalir, A., Elkavets, R., Maayani, S., Rehavi, M., Sokolovsky, M., Pri-Bar, I., & Buchman, O. (1978). Structure-activity relationship of some phencyclidine derivatives: in vivo studies in mice. European Journal of Medicinal Chemistry, 13(1), 17-24.

References

  1. 1.0 1.1 1.2 1.3 Itzhak, Y., Kalir, A., & Sarne, Y. (1981). On the opioid nature of phencyclidine and its 3-hydroxy derivative. European Journal of Pharmacology, 73(2-3), 229-233.
  2. 2.0 2.1 2.2 Kalir, A., Elkavets, R., Maayani, S., Rehavi, M., Sokolovsky, M., Pri-Bar, I., & Buchman, O. (1978). Structure-activity relationship of some phencyclidine derivatives: in vivo studies in mice. European Journal of Medicinal Chemistry, 13(1), 17-24.
  3. Morris, H., & Wallach, J. (2014). From PCP to MXE: A comprehensive review of the non-medical use of dissociative drugs. Drug Testing and Analysis, 6(7–8), 614–632. https://doi.org/10.1002/dta.1620
  4. Beagle, J. Q. (1999). Structure Activity of PCP analogs. Retrieved from https://erowid.org/archive/rhodium/chemistry/pcp/sar.html#sarphenyl
  5. Morris, H., & Wallach, J. (2014). From PCP to MXE: A comprehensive review of the non-medical use of dissociative drugs. Drug Testing and Analysis, 6(7–8), 614–632. https://doi.org/10.1002/dta.1620
  6. "(ACMD) Methoxetamine Report (2012)" (PDF). UK Home Office. 2012-10-18. p. 14. Retrieved 2015-06-24.
  7. Fusar-Poli, P., Crippa, J. a, Bhattacharyya, S., Borgwardt, S. J., Allen, P., Martin-Santos, R., … McGuire, P. K. (2009). Distinct effects of {delta}9-tetrahydrocannabinol and cannabidiol on neural activation during emotional processing. Archives of General Psychiatry, 66(1), 95–105. http://doi.org/10.1001/archgenpsychiatry.2008.519
  8. Doyle, O. M., De Simoni, S., Schwarz, a J., Brittain, C., O’Daly, O. G., Williams, S. C. R., & Mehta, M. a. (2013). Quantifying the attenuation of the ketamine pharmacological magnetic resonance imaging response in humans: a validation using antipsychotic and glutamatergic agents. The Journal of Pharmacology and Experimental Therapeutics, 345(1), 151–60. http://doi.org/10.1124/jpet.112.201665
  9. Gisselgård, J., Anda, L. G., Brønnick, K., Langeveld, J., Ten Velden Hegelstad, W., Joa, I., … Larsen, T. K. (2014). Verbal working memory deficits predict levels of auditory hallucination in first-episode psychosis. Schizophrenia Research, 153(1–3), 38–41. http://doi.org/10.1016/j.schres.2013.12.018
  10. 3-HO-PCP (Tripsit) | https://wiki.tripsit.me/wiki/3-HO-PCP
  11. The Misuse of Drugs Act 1971 (Amendment) Order 2013 (Legislation.gov.uk) | http://www.legislation.gov.uk/uksi/2013/239/introduction/made