The science of alpha-PVP (“gravel”), a second-generation bath salt

March 14, 2014, 7:24 pm

★★★½☆

Pharmacology of novel synthetic stimulants structurally related to the “bath salts” constituent 3,4-methylenedioxypyrovalerone (MDPV). Marusich JA at al. Neuropharmacology 2014 Mar2 [Epub ahead of print]

Abstract

Earlier this month TPR noted that a relatively new second-generation bath salt call “gravel” was reported to have surfaced in various parts of the United States, including Tennessee. As background, while first-generation bath salts — MDPV, methylone, and mephedrone — were outlawed in many jurisdictions, new analogues had been introduced to replace them and were still generally legal. Samples of “gravel” contained α-PVP, an analogue of MDPV. It seemed to produce impressive degrees of paranoia. Some samples of the drug were adulterated with methamphetamine and/or clonazepam.

This current study just posted online is thus a timely and important contribution to understanding this new drug. Using an in vivo and in vitro rat model, the authors sought to compare the effects of MDPV with those of its analogues, including α-PVP.

Like MDPV, α-PVP contains a pyrrolidine ring, a 5-sided nitrogen-containing component that enables the molecule to effectively block reuptake of dopamαine and norepinephrine, with much weaker effects at the serotonin transporter.

In rats, α-PVP produced evidence of psychomotor stimulation, with higher doses causing hyperactivity and bizarre behavior. A dopamine antagonist blocked much of the motor hyperactivity.

Although I tend to shy away from rat studies, I found this one important because it is one of the first studies of the effects of α-PVP (aka “gravel”).

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