Pyrrolidinophenones (pyrovalerones) for sale


Pyrrolidinophenones (pyrovalerones)—synthetic psychostimulants and research chemicals of the cathinones class, is a desmethyl analogue of pyrovalerone.

Metabolism

Metabolism proceeds with the processes involvement of acetylation and glucuronide conjugation.

The presence of the pyrrolidone ring causes certain features of the toxicokinetics and metabolism of pyrrolidinophenones. Thus, pyrrolidinophenones exceed other cathinones by their ability to overcome the blood-brain barrier (BBB), but they are inferior to amphetamine-type stimulants in this indicator. The main pathways of pyrrolidinophenones metabolism:

  • ketone group reduction with the alcohol formation;
  • hydroxylation in 2nd position of the pyrrolidine ring, followed by oxidation to lactam;
  • hydroxylation of the 4-methyl group followed by carboxylation.

This metabolism pathway is characteristic of 4-methyl-a-pyrrolidinopropiophenone, 4-methyl-a-pyrrolidinobutiophenone, pyrovalerone, methyl-a-pyrrolidinohexiophenone, i.e. for drugs that have a methyl radical in the 4-position of the aromatic ring.

  • demethylation of the 4-methoxy group to 4-hydroxy metabolite form (for 4-methoxy-a-pyrrolidinopropiophenone, 4-methoxy-a-pyrrolidinobutiophenone, 4-methoxypyraloperone, 4-methoxy-a-pyrrolidinohexiophenone);
  • demethylation of the 3,4-methylenedioxy group, followed by methylation 3 or 4-hydroxyl (for 3,4-methylenedioxy-a-pyrrolidinopropiophenone, 3,4-methylenedioxy-a-pyrrolidinobutiophenone, 3,4-methylenedioxypiperovalonone, 3,4-methylenedioxy-a-pyrrolidinohexiophenone);
  • conjugation proceeds by the type of acetylation, binding with glucuronic acid and with sulfates.

There are metabolism features of various pyrrolidinophenones.

Attempts have been made to evaluate the biotransformation patterns of synthetic cathinones in humans. In humans, the metabolism processes of cathinone are best studied, since the period of research covers several decades.

Pharmacology and effects

Inhibition of DAT, SERT, and NET is accompanied by a monoamine reagent weakening and an increase in their concentration in the synaptic cleft. This activation path is similar to the mechanism of action of cocaine—this psychostimulant blocks the reverse capture of predominantly dopamine and norepinephrine.

Pyrrolidinophenones can act as substrates for monoamine transport systems (DAT, NET and SERT). After interaction with the transporter, the agent is translocated to the presynaptic termination and induces a reversible monoamine transport (i.e., the transport system starts to pump the neurotransmitter from the presynaptic space to the synaptic cleft). Such substances are commonly referred to as releasers. A similar toxicity mechanism is characteristic of amphetamine, methamphetamine and MDMA.

Finally, pharmacological activity mechanism of pyrrolidinophenones is the inhibition of the neurotransmitter-monoamine transport system into synaptic vesicles (VMAT2 system). As a result, monoamines accumulate in the cytoplasm of the presynaptic end, which facilitates their subsequent release into the synaptic cleft.

Depending on the neurochemical profile, pyrrolidinophenones can be distributed into the following groups:

  • pyrrolidinophenones, which are nonselective inhibitors of monoamine transport systems, ie, by the mechanism of action they resemble cocaine (mephedrone, methylone, ethylone, butylone, naphyrone). Naphyrone also exhibits serotonin releaser properties, which brings it closer to MDMA;
  • pyrrolidinophenones resembling methamphetamine (cathinone, methcathinone, flephedrone). Inhibit monoamine reagent systems and enhance the dopamine release (ie, they are dopamine releases);
  • pyrovalerone and methylenedioxypyrovalerone are potent and selective inhibitors of the reagent dopamine and norepinephrine and do not possess the monoamine release agents properties.

The clinical effects of pyrrolidinophenones and classical psychostimulants are similar: after taking drugs, thinking speeds up, motor activity increases, a sense of euphoria appears, and sexual attraction increases. Acceleration of intoxication is accompanied by the addition of hallucinations, paranoia, insomnia, agitation, suicidal thoughts. Signs of sympathomimetic action are mydriasis, tachycardia, hypertension. Cases of seizures, serotonin syndrome, rhabdomyolysis, kidney damage and other complications were noted.


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