General Information

Methylenedioxypyrovalerone (MDPV), also known as monkey dust, is a stimulant belonging to the cathinone class, functioning as a norepinephrine-dopamine reuptake inhibitor (NDRI). It was initially synthesized in the 1960s by researchers at Boehringer Ingelheim. MDPV’s effect on the dopamine transporter is approximately six times more potent than its effect on the norepinephrine transporter, and it shows almost no activity at the serotonin transporter. This stimulant remained relatively unknown until about 2004, when it started being sold as a designer drug. In the United States, MDPV-containing products, marketed as bath salts, were sold as recreational drugs in gas stations, much like how Spice and K2 were promoted as incense, until its ban in 2011.

MDPV Physico-Chemical Properties

MDPV hydrochloride (CAS 24622-62-6) is a white to light brown crystalline powder that is soluble in water and organic solvents like ethanol. Its chemical formula is C16H21NO3 · HCl, with a molecular weight of 311.80 g/mol. The compound has a melting point of around 238–239°C. MDPV hydrochloride is known for its high stability, which contributes to its persistence in the environment and the human body.

Chemically, MDPV is a derivative of pyrovalerone (a-PVP), differing by the addition of a 3,4-methylenedioxy group to the phenyl ring. This modification increases the compounds lipophilicity, allowing it to cross the blood-brain barrier more effectively and rapidly, leading to its potent central nervous system (CNS) stimulant effects.

MDPV Hydrochloride Solubility

• 0.9% NaCl: 20 mg/ml
• DMF: 0.25 mg/ml
• DMSO: 0.1 mg/ml
• Ethanol: 1 mg/ml

• PBS (pH 7.2): 10 mg/ml

MDPV Synthesis

Synthesis way is similar with a-PVP synthesis and can be done in two step from 1-(benzo[d][1,3]dioxol-5-yl)pentan-1-one (CAS 63740-98-7).

α-PVP/MDPV hydrochloride synthesis (Full)

MDPV Application

MDPV was never approved for medical use, and its application has been largely restricted to recreational and illicit contexts. Initially, MDPV was marketed as a research chemical or a component of so-called “bath salts,” which were sold legally in some areas before the substance was widely recognized for its harmful psychoactive effects.

In recreational settings, MDPV is often used for its stimulant effects, which include increased alertness, energy, and euphoria.

MDPV Pharmacology

MDPV is believed to function mainly as a powerful norepinephrine-dopamine reuptake inhibitor. By reducing the reuptake of norepinephrine and dopamine, it leads to increased levels of these two catecholamine neurotransmitters in the synaptic cleft, which is the space between neurons.

This inhibition results in heightened and prolonged concentrations of these neurotransmitters, enhancing their post-synaptic effects on dopamine and norepinephrine receptors in the receiving neuron. While serotonin also plays a role, its involvement is much less significant. This rapid surge in neurotransmitter levels in the brain is thought to be what causes the euphoric effects associated with MDPV.

Since MDPV primarily inhibits reuptake rather than releasing neurotransmitters, its mechanism of action is more similar to that of cocaine or methylphenidate than to amphetamines. In contrast, amphetamines mainly act by indirectly releasing dopamine and norepinephrine through the activation of the TAAR1 receptor.

Effects and Symptoms of MDPV Use

Physical effects

• Stimulation
• Stamina enhancement
• Abnormal heartbeat
• Increased heart rate – Higher doses of MDPV can create a significant and often dangerous increase in heart rate and blood pressure.
• Muscle contractions
• Muscle spasms
• Appetite suppression
• Headaches
• Gustatory hallucinations
• Diarrhea – Some users have reported experiencing diarrhea while under the influence of MDPV, although this seems to be a relatively uncommon effect.
• Nausea – Some users have reported experiencing nausea while under the influence of MDPV, although this seems to be a relatively uncommon effect.
• Restless leg syndrome
• Auditory effects
• Auditory distortion
• Auditory hallucination

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. Its effects commonly include:

• Anxiety
• Cognitive fatigue
• Depression
• Irritability
• Motivation suppression
• Thought deceleration
• Wakefulness

It should be noted that many users consider the after effects of MDPV to be significantly more unpleasant if compulsively redosed.

Cognitive effects

The general cognitive effects of MDPV can be described as being similar to those of other typical stimulants. At common dosages, the MDPV high is described as being euphoric and slightly empatheogenic in its effects, causing increased motivation, sociability, sexual desire and concentration. Higher doses of MDPV, however, can intensify numerous negative effects such as anxiety and disorganized thoughts; at extremely high doses or continued use, delusions and psychosis become likely.

• Anxiety
• Cognitive euphoria
• Compulsive redosing – MDPV is extremely potent in this effect; it has been shown that some users end up redosing, even if the negative effects outweigh the positives.
• Confusion – This effect is prominent at higher doses and after long periods of staying awake on the drug.
• Creativity enhancement
• Delusions – This effect can also manifest at high doses.
• Ego inflation
• Empathy, love, and sociability enhancement – MDPV’s effects in this regard are similar to, but weaker than, those of MDMA.
• Focus enhancement
• Increased libido
• Motivation enhancement
• Paranoia
• Stamina enhancement
• Psychosis – High doses of MDPV have been known to induce states of psychosis at a more frequent rate than most other stimulants.
• Time distortion – This can be described as the experience of time speeding up and passing much quicker than it usually would when sober.
• Thought acceleration
• Thought organization – Mainly observed with low to common doses.
• Thought disorganization – This effect manifests and is also intensified at higher doses.
• Wakefulness – Strong wakefulness is reported at high doses and can last for many hours after long periods of use.

Dosage

• Threshold 2 mg
• Light 4 – 8 mg
• Common 8 – 14 mg
• Strong 14 – 25 mg
• Heavy 25 mg +

Duration

• Total 2 – 7 hours
• Onset 15 – 30 minutes
• Peak 1 – 4 hours
• Offset 0.5 – 2 hours
• After effects 2 – 48 hours

MDPV Legal Status

Due to its harmful effects and lack of medical utility, MDPV has been classified as a controlled substance in many countries around the world. In the United States, MDPV was added to the Schedule I list of controlled substances in 2011, making its production, distribution, and possession illegal. Similarly, the European Union and other regions have also banned MDPV, classifying it under various drug control laws to curb its spread and misuse.

The legal status of MDPV means that it is illegal to manufacture, distribute, or possess the substance without proper authorization, typically limited to certain scientific research contexts under strict regulatory oversight.

Conclusion

MDPV, with its potent stimulant properties, has garnered significant interest for its unique effects on the central nervous system. Its ability to increase alertness, energy, and focus has made it a compound of interest in various scientific studies exploring its potential applications. Its physico-chemical properties and synthesis pathways provides valuable insights that could inform future research in pharmacology and neuroscience. While its use must be approached with caution due to its potency, Mdpv distinct characteristics continue to contribute to ongoing discussions in the scientific community about its potential benefits and uses.

Bibliography

• Coppola, M., and R. Mondola. “3, 4-methylenedioxypyrovalerone (MDPV): chemistry, pharmacology and toxicology of a new designer drug of abuse marketed online.” Toxicology letters 208.1 (2012): 12-15. https://doi.org/10.1016/j.toxlet.2011.10.002
• https://bbgate.com/threads/synthesis-of-synthetic-cathinones.214/
• https://psychonautwiki.org
• https://www.narconon.org