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| Summary sheet: A-PiHP |
| A-PiHP | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Chemical Nomenclature | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Common names | α-PiHP α-PHiP | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Substitutive name | 4-Methyl-1-phenyl-2-(pyrrolidin-1-yl)pentan-1-one | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Systematic name | alpha-Pyrrolidinoisohexanophenone | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Class Membership | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Psychoactive class | Stimulant | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Chemical class | Cathinone / Pyrrolidinophenone | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Routes of Administration | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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alpha-Pyrrolidinohexiophenone (also known as α-PihP, and 4-methyl-alpha-pyrrolidinopentanophenone) is a lesser-known novel stimulant substance of the cathinone and pyrrolidinophenone classes. It is structurally related to MDPV and A-PHP and is one of the latest successors to the designer drug cathinone analog A-PVP|α-PVP].
Subjective effects such as euphoria, thought acceleration, disinhibition and ego inflation. It generally comes in the form of either a fine powder or crystallized shards that can produce powerful but short-lived euphoric stimulant effects reported to be more compulsive in nature (and strength) to vaporized methamphetamine. Like its cathinone predecessors, it is has gained notoriety for its tendency to induce compulsive redosing and addictive behaviors as well the ability to produce delusional states and psychosis when abused. The compulsivity induced in A-PiHP seems to be stronger compared to similar substances in this class, as reported by online anecdotal reports.
Very little data exists about the pharmacological properties, metabolism, and toxicity of α-PiHP. It has recently become commonly marketed as a legal, grey-market alternative to A-PHP, 3-MMC, and A-PVP, and commercially distributed through online research chemical vendors.
It is highly advised to use harm reduction practices if using this substance.
Chemistry
α-PHiP (also known as α-PiHP), is a stimulant drug of the cathinone class. It is a positional isomer of pyrovalerone, with the methyl group shifted from the 4-position of the aromatic ring to the 4-position of the acyl chain. In a classic 2006 study of pyrrolidinyl cathinone derivatives by Meltzer et al. at Organix, the alpha-isobutyl derivative of pyrovalerone, O-2494, was found to have the highest potency in vitro as an inhibitor of the dopamine transporter of the alpha substituted derivatives tested, however it was not until ten years later in July 2016 that α-PHiP was first identified as a designer drug, when it was reported to the EMCDDA by a forensic laboratory in Slovenia.
Pharmacology
The mechanism of action of α-PiHP is unknown. Aside from a substantially shorter duration, it is believed to act similarly to the designer drug pentedrone and α-PVP, which both act as a potent norepinephrine-dopamine reuptake inhibitors (NDRI) without being neurotransmitter releasers,[1] although no substantial research on the pharmacology of this compound has yet been conducted.
This means it may effectively boost the levels of the norepinephrine and dopamine neurotransmitters in the brain by binding to and partially blocking the transporter proteins that normally remove those monoamines from the synaptic cleft. This allows dopamine and norepinephrine to accumulate within the brain, resulting in stimulating and euphoric effects.
Subjective effects
This compound is reported to be similar to A-PHP. More information needed.
Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.
It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.
Physical effects 
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- Stimulation - α-PiHP can be considered to be extremely stimulating and energetic, although less so than α-PVP. This encourages activities such as running, climbing and dancing, although it can also encourage sitting immobile and engaging in repetitive tasks. The particular style of stimulation which α-PiHP presents can be described as forced. This means that at higher dosages it becomes difficult or impossible to keep still as jaw clenching, involuntarily bodily shakes and vibrations become present, resulting in an extreme unsteadiness of the hands and a general lack of motor control.
- Spontaneous physical sensations - The "body high" of α-PiHP can be described as a moderate to extreme euphoric tingling sensation that encompasses the entire body. It is capable of becoming overwhelming at higher dosages. This sensation maintains a consistent presence that steadily rises with the onset and hits its limit once the peak has been reached.
- Tactile enhancement - α-PiHP can enhance one's sense of touch to extreme degrees, often leading to states of sexual arousal.
- Vibrating vision - A person's eyeballs may begin to spontaneously wiggle back and forth in a rapid motion, causing vision to become blurry and temporarily out of focus (a condition known as nystagmus).
- Appetite suppression
- Focus enhancement - α-PiHP has been noted as enhancing focus, but in a way that leaves the user totally fixated on whatever task at hand, however trivial.
- Mouth numbing - In a similar fashion to that of cocaine this compound numbs the areas of the body which it touches, these areas can include the nostrils, gums, mouth and throat of the user.
- Abnormal heartbeat - Due to the potency of its rush, α-PiHP can cause various uncomfortable or painful sensations in the heart, especially when abused or used for extended periods. Those with familial or personal heart issues are discouraged from using this drug in its most potent routes of administration.
- Increased blood pressure - α-PiHP, especially when it is vaporized or injected, can lead to sudden spikes of blood pressure that may manifest in an extremely uncomfortable "exploding heart" sensation.
- Increased heart rate
- Dehydration - Dry mouth and dehydration are a universal experience with α-PiHP and are a product of an increased heart rate, adrenergic activity and the motivation to engage in strenuous physical activities. While it is important to avoid becoming dehydrated, especially when out dancing in a hot environment, there is a potential possibility of suffering from water intoxication through over-drinking. Therefore it is advised that users simply sip at water and be mindful of their water in-take.
- Dry mouth
- Difficulty urinating - Higher doses of α-PiHP result in an overall difficulty when it comes to urination, an effect that is temporary and typically harmless.
- Headaches - This typically can occur towards the end of the experience, but can sometimes happen during one as well.
- Increased perspiration
- Muscle spasms
- Restless leg syndrome
- Vasoconstriction - α-PiHP can be considered very vasoconstricting at higher doses, and is described as stronger than that of amphetamine and methamphetamine.
- Teeth grinding - This component can be considered to be less intense when compared with that of MDMA, though becomes more present at high doses.
- Seizure - α-PiHP may lower the seizure threshold in some individuals, especially when it is misused.
Visual effects 
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- Brightness alteration - α-PiHP can make spaces seem brighter due to its ability to dilate the pupils.
- Drifting - This effect is usually very mild and increases with sleep deprivation.
- Visual acuity suppression - α-PiHP can have visual and vision-impairing effects that can lend readily to peripheral hallucinations.
Hallucinatory states
Cognitive effects 
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The cognitive effects of α-PiHP can be broken down into several components which progressively intensify proportional to dosage. The ample head space of α-PiHP is described by many as one of extreme mental stimulation and powerful euphoria. It contains a large number of typical stimulant cognitive effects, particularly those of the cathinone or pyrrolidine classes of drugs.
The most prominent of these cognitive effects generally include:
- Disinhibition
- Cognitive euphoria - A euphoria very similar to amphetamine or cocaine is present as well as feelings of joy and happiness which are likely a direct result of marked norepinephrine and dopamine reuptake inhibition.
- Analysis enhancement - Users report that this effect typically only occurs at low doses, and becomes increasingly more impairing as one increases their intake.
- Anxiety & Paranoia - α-PiHP can lead to states of extreme anxiety and paranoia when dosed too highly or frequently, which is why eyeballing this substance is strongly discouraged. The anxiety and paranoia this compound produces shares many features of the paranoia that can be induced by methamphetamine or cocaine, and typically happens during the come down phase of the experience.
- Feelings of impending doom - This typically is experienced when the substance is abused, but can happen at higher than needed doses, or the comedowns of binges. It can also happen spontaneously, although this tends to be rare.
- Information processing suppression
- Ego inflation - Similar to the ego inflation of cocaine or methamphetamine, α-PiHP can temporarily induce states of egomania at its peak.
- Compulsive redosing - Reported to be unusually strong, moreso than A-PHP. Users are advised to use extreme caution in not losing control when on this drug.
- Immersion enhancement
- Motivation enhancement - This effect provides short-lived states of extreme motivation, but due to the cognitively narrowing aspects of its action, rarely ever translates into productive action.
- Increased libido - α-PiHP, like its predecessor A-PHP, can induce states of extreme sexual arousal due to its powerful disinhibiting effects
- Increased music appreciation
- Thought acceleration
- Time distortion - Strong feelings of time compression are common within α-PiHP and increase in the perception of perceived experience is greatly increased
- Wakefulness
Auditory effects 
Multi-sensory effects 
After effects 
- The effects which occur during the offset of a stimulant experience generally feel negative and uncomfortable in comparison to the effects which occurred during its peak. This is often referred to as a "comedown" and occurs because of neurotransmitter depletion. It has been reported that this crash is usually not considered as severe as it is on A-PVP at equivalent dosages. The effects commonly include, but are not limited to:
Toxicity and harm potential
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This toxicity and harm potential section is a stub. As a result, it may contain incomplete or even dangerously wrong information! You can help by expanding upon or correcting it. |
The toxicity and long-term health effects of recreational α-PiHP use do not seem to have been studied in any scientific context and the exact toxic dosage is unknown. This is because α-PiHP has very little history of human usage.
α-PiHP has been reported to be the cause of death in one individual. Due to the similarity of structures and the reported dosages, an attempt to compare the concentrations of α-PVP and α-PHP has been made. In the described case, functional death through intoxication of α-PiHP was accepted as the final cause of death. Other detected substances did not contribute to death due to their very likely distant administration. [2]
It is strongly recommended that one use harm reduction practices when using this substance.
Tolerance and addiction potential
As with other short-lived highly dopaminergic stimulants, the chronic use of α-PiHP can be considered highly addictive with a high potential for abuse and is capable of causing psychological dependence among certain users. When addiction has developed, cravings and withdrawal effects may occur if a person suddenly stops their usage.
Tolerance to many of the effects of α-PiHP develops with prolonged and repeated use. This results in users having to administer increasingly large doses to achieve the same effects. After that, it takes about 3 - 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). α-PiHP presents cross-tolerance with all dopaminergic stimulants, meaning that after the consumption of α-PiHP all stimulants will have a reduced effect.
Psychosis
α-PiHP, like other strongly dopaminergic stimulants, can result in a stimulant psychosis that may present with a variety of symptoms (e.g., paranoia, hallucinations, or delusions).[3][4] A review on treatment for amphetamine, dextroamphetamine, and methamphetamine abuse-induced psychosis states that about 5–15% of users fail to recover completely.[5][6] The same review asserts that, based upon at least one trial, antipsychotic medications effectively resolve the symptoms of acute amphetamine psychosis.[7]
Dangerous interactions
Warning: Many psychoactive substances that are reasonably safe to use on their own can suddenly become dangerous and even life-threatening when combined with certain other substances. The following list provides some known dangerous interactions (although it is not guaranteed to include all of them).
Always conduct independent research (e.g. Google, DuckDuckGo, PubMed) to ensure that a combination of two or more substances is safe to consume. Some of the listed interactions have been sourced from TripSit.
- 25x-NBOMe & 25x-NBOH - 25x compounds are highly stimulating and physically straining. Combinations with A-PiHP should be strictly avoided due to the risk of excessive stimulation and heart strain. This can result in increased blood pressure, vasoconstriction, panic attacks, thought loops, seizures, and heart failure in extreme cases.
- Alcohol - Combining alcohol with stimulants can be dangerous due to the risk of accidental over-intoxication. Stimulants mask alcohol's depressant effects, which is what most people use to assess their degree of intoxication. Once the stimulant wears off, the depressant effects will be left unopposed, which can result in blackouts and severe respiratory depression. If mixing, the user should strictly limit themselves to only drinking a certain amount of alcohol per hour.
- DXM - Combinations with DXM should be avoided due to its inhibiting effects on serotonin and norepinephrine reuptake. There is an increased risk of panic attacks and hypertensive crisis, or serotonin syndrome with serotonin releasers (MDMA, methylone, mephedrone, etc.). Monitor blood pressure carefully and avoid strenuous physical activity.
- MDMA - Any neurotoxic effects of MDMA are likely to be increased when other stimulants are present. There is also a risk of excessive blood pressure and heart strain (cardiotoxicity).
- MXE - Some reports suggest combinations with MXE may dangerously increase blood pressure and increase the risk of mania and psychosis.
- Dissociatives - Both classes carry a risk of delusions, mania and psychosis, and these risk may be multiplied when combined.
- Stimulants - A-PiHP may be dangerous to combine with other stimulants like cocaine as they can increase one's heart rate and blood pressure to dangerous levels.
- Tramadol - Tramadol is known to lower the seizure threshold[8] and combinations with stimulants may further increase this risk.
Serotonin syndrome risk
Combinations with the following substances can cause dangerously high serotonin levels. Serotonin syndrome requires immediate medical attention and can be fatal if left untreated.
- MAOIs - Such as banisteriopsis caapi, syrian rue, phenelzine, selegiline, and moclobemide.[9]
- Serotonin releasers - Such as MDMA, 4-FA, methamphetamine, methylone and αMT.
- SSRIs - Such as citalopram and sertraline
- SNRIs - Such as tramadol and venlafaxine
- 5-HTP
Legal status
- Brazil: As of September 7, 2018, all cathinone analogues are controlled substances considered illegal to possess, use and distribute. This was made possible due to a blanket ban law appended to Portaria SVS/MS nº 344.[10]
- Canada: α-PiHP is a Schedule 1 drug in Canada.
- Estonia:α-PiHP is a I Schedule drug and was officially banned on September 4, 2023. Before that date, α-PiHP would have just fallen under VI Schedule cathinone blanket ban.[11]
- Italy: The President of the Republic of Italy classified cathinone and all structurally derived analogues (including pyrovalerone analogues) as Narcotics in January 2012. [12]
- United Kingdom: is a Class B drug in the United Kingdom as a result of the cathinone catch-all clause.[13]
- United States: α-PiHP has been assigned to Schedule I on a Temporary Placement basis. This order, which extends the temporary scheduling order that DEA previously issued for these substances (84 FR 34291, July 18, 2019), is effective July 18, 2021 and expires on July 18, 2022. .[14] As such, the sale or the use of this compound is prohibited.
See also
External links
References
- ↑ http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2602954
- ↑ (PubMed) | https://pubmed.ncbi.nlm.nih.gov/31751796/
- ↑ http://www.drugabuse.gov/drugs-abuse/emerging-trends
- ↑ Treatment for amphetamine psychosis | [1]
- ↑ Treatment for amphetamine psychosis | [2]
- ↑ Hofmann FG (1983). A Handbook on Drug and Alcohol Abuse: The Biomedical Aspects (2nd ed.). New York: Oxford University Press. p. 329. ISBN 9780195030570.
- ↑ Treatment for amphetamine psychosis | [3]
- ↑ Talaie, H.; Panahandeh, R.; Fayaznouri, M. R.; Asadi, Z.; Abdollahi, M. (2009). "Dose-independent occurrence of seizure with tramadol". Journal of Medical Toxicology. 5 (2): 63–67. doi:10.1007/BF03161089. eISSN 1937-6995. ISSN 1556-9039. OCLC 163567183.
- ↑ Gillman, P. K. (2005). "Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity". British Journal of Anaesthesia. 95 (4): 434–441. doi:10.1093/bja/aei210
. eISSN 1471-6771. ISSN 0007-0912. OCLC 01537271. PMID 16051647.
- ↑ New blanket ban on synthetic illegal drugs is approved (Portuguese) | http://portal.anvisa.gov.br/noticias/-/asset_publisher/FXrpx9qY7FbU/content/combate-a-drogas-ilicitas-sinteticas-fica-mais-facil/219201/pop_up?_101_INSTANCE_FXrpx9qY7FbU_viewMode=print&_101_INSTANCE_FXrpx9qY7FbU_languageId=pt_BR
- ↑ https://www.riigiteataja.ee/akt/128022023013?leiaKehtiv (Estonian)
- ↑ http://www.politicheantidroga.it/media/491607/decreto%20ministero%20salute%2029%20dicembre%202011.pdf
- ↑ United Kingdom. (2010). Misuse of Drugs Act 1971 (S.I. 2010/1207). London: The Stationery Office Limited. Retrieved February 9, 2018, from https://www.legislation.gov.uk/uksi/2010/1207/made
- ↑ {{cite web | title = Schedules of Controlled Substances Extension | url = https://www.federalregister.gov/documents/2021/07/16/2021-15113/schedules-of-controlled-substances-extension-of-temporary-placement-of-n | publisher = Drug Enforcement Administration | access-date = 2022-04-22 |.