Description
alpha-Pyrrolidinovalerophenone (also known as α-PVP, A-PVP, alpha-PVP, and flakka) is a novel stimulant substance of the cathinone class. α-PVP is chemically related to prolintane and belongs to a group called the substituted cathinones, which includes compounds like MDPV, hexen, and a-PHP. It acts as a norepinephrine-dopamine reuptake inhibitor.
α-PVP was patented in the 1960s by Boehringer Ingelheim,. although it was never marketed. Reports of its use began to appear in the early 2010s. α-PVP has been subject to much scrutiny by the media as one of the ingredients found in “bath salts” or “legal highs” products.[. It has been mass produced in China and sold online as a research chemical.[. It has been linked to numerous hospitalizations and overdose deaths..
User reports indicate that α-PVP produces powerful but short-lived stimulant effects comparable to those of methamphetamine and cocaine when insufflated or vaporized. Commonly reported effects include stimulation, disinhibition, increased libido, compulsive redosing, and euphoria. Like other synthetic cathinones, α-PVP is associated with compulsive use and addiction.
Very little data exists about the pharmacological properties, metabolism, and toxicity of a-PVP. Due to its potent psychostimulant effects and unknown toxicity profile, it is highly advised to use harm reduction practices if using with this substance.
Chemistry
α-PVP, or alpha-Pyrrolidinovalerophenone, is a synthetic substance belonging to a group called the substituted cathinones. Substituted cathinones are derivatives of the naturally occurring substance cathinone, which is one of the psychoactive principles in khat (Catha edullis). Cathinone is composed of a phenethylamine core with an alkyl group attached to the alpha carbon, and a ketone group attached to the beta carbon. α-PVP’s structure consists of a cathinone core with a propyl group substituted at the alpha carbon, and a pyrrolidine ring at the amino group.
The hydrochloride salt of α-PVP is described as a white or off-white, odourless crystalline powder, with a melting point of 161.3°C. It is reported to be soluble in PBS (~10mg/ml, pH7.2), in EtOH (~20mg/ml), in DMSO (~10mg/ml) and in DMF (~3mg/ml)..
Pharmacology
α-PVP is a potent and selective norepinephrine–dopamine reuptake inhibitor (NDRI), with a similar potency as MDPV.. α-PVP does not act as a transporter substrate, i.e. it does not cause neurotransmitter release. It is a more potent inhibitor of DAT and NET than the classical stimulants cocaine and amphetamine.
Compound | DAT (nM) | NET (nM) | SERT (nM) | DAT/SERT ratio |
---|---|---|---|---|
a-PVP | 12.8 ± 1.2 | 14.2 ± 1.2 | >10,000 | >781 |
MDPV | 4.1 ± 0.6 | 25.9 ± 5.6 | 3305 ± 485 | 806 |
Cocaine | 211 ± 19 | 292 ± 34 | 313 ± 17 | 1.5 |
Amphetamine | 93 ± 17 | 67 ± 16 | 3418 ± 314 | 37 |
Dosage | |
---|---|
Threshold | 1 – 2 mg |
Light | 2 – 5 mg |
Common | 5 – 15 mg |
Strong | 15 – 25 mg |
Heavy | 25 mg + |
Duration | |
Total | 30 – 60 minutes |
Onset | 20 – 60 seconds |
Peak | 3 – 6 minutes |
Offset | 15 – 30 minutes |
After effects | 1 – 3 hours |
ExpandOral |
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CollapseInsufflated | |
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Dosage | |
Threshold | 0.5 – 1 mg |
Light | 1 – 5 mg |
Common | 5 – 15 mg |
Strong | 15 – 25 mg |
Heavy | 25 mg + |
Duration | |
Total | 2 – 5 hours |
Onset | 10 – 30 minutes |
Peak | 20 – 45 minutes |
Offset | 30 – 90 minutes |
After effects | 2 – 4 hours |
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