Pentedrone

Pentedrone is a molecule of the substituted cathinone chemical class. Substituted cathinones refer to a class of molecules which are principally constituted of a phenethylamine core with an alkyl group attached to the alpha carbon and an oxygen group attached to the beta carbon. They are also known as the beta-ketone (double-bonded oxygen to the β-carbon) analogs of amphetamines. Pentedrone is the a-pentyl beta-keto analog of methamphetamine.

Of general note, the cathinone backbone can be modified in three different places to create hundreds of possible compounds, which include substituents on the aromatic ring, the alpha carbon, and the amine group.^[3]

Due to the lack of research regarding the substance, all proceeding discussion regarding the pharmacology of this compound derives from speculation based upon its structure and subjective effect similarities to other cathinones and related molecules, such as prolintane, a-PVP, a-PHP and analogs like N-ethyl-(nor)-pentedrone (i.e. NEP).

Unlike many other substituted cathinones, which display both reuptake-inhibition and releasing agent properties, pentedrone has been shown to act as a pure reuptake inhibitor for the major catecholamine neurotransmitters dopamine and norepinephrine, with very modest activity on serotonin. This renders its pharmacological activity similar to that of methylphenidate, cocaine or MDPV (although the latter two possess heavy additional serotonergic activity. These pure uptake inhibitors likely do not enter the intracellular space of the synapse via the transporter, which may be associated with less intracellular pharmacological effects and toxicity compared with substrate-type releasers^[1]This enables the endogenous neurotransmitters dopamine and norepinephrine to accumulate within various synaptic regions in the brain, resulting in stimulating and euphoric effects.^{[citation needed]}

Notably, the addition of an ethyl group to the terminal amine (-NH2) group of the pentedrone molecule seems to increase its potency significantly, as is observed with its successor analog N-ethyl-(nor)-pentedrone (i.e. NEP) which is viewed as having preferential recreational properties.

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 ☠.

Experience reports

Anecdotal reports which describe the effects of this compound within our experience index include:

• Experience:A combination of DOC, 5-MAPB, 5-MeO-DMT, ETH-LAD, Cannabis, Pentedrone

Additional experience reports can be found here:

• Erowid Experience Vaults: Pentedrone

The toxicity and long-term health effects of recreational pentedrone use do not seem to have been studied in any scientific context and the exact toxic dosage is unknown. This is because pentedrone has a very short history of human usage. Early anecdotal evidence from people who have tried pentedrone within the community suggests that there do not seem to be any negative health effects attributed to simply trying this substance at low to moderate doses by itself and using it in a sparing and controlled fashion (but nothing can be completely guaranteed).

It is strongly recommended that one use harm reduction practices when using this substance.

Tolerance and addiction potential

As with other stimulants, the chronic use of pentedrone can be considered moderately addictive with a high potential for abuse and seems to be readily liable 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 pentedrone 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 total absence of further consumption). Pentedrone presents cross-tolerance with all dopaminergic stimulants, meaning that after the consumption of pentedrone all stimulants will have a reduced effect.

Psychosis

Abuse of compounds within the stimulant class at high dosages for prolonged periods of time can potentially result in a stimulant psychosis that may present with a variety of symptoms (e.g., paranoia, hallucinations, or delusions).^[4] A review on treatment for (dextro)amphetamine, and methamphetamine abuse-induced psychosis states that about 5–15% of users fail to recover completely.^[4][5] The same review asserts that, based upon at least one trial, antipsychotic medications effectively resolve the symptoms of acute amphetamine psychosis.^[4]

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.

• Stimulants - Pentedrone can be potentially dangerous in combination with other stimulants as it can increase one's heart rate and blood pressure to dangerous levels.
• 25x-NBOMe & 25x-NBOH - 25x compounds are highly stimulating and physically straining. Combinations with Pentedrone 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 - Pentedrone 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^[6] and combinations with stimulants may further increase this risk.
• MDMA - The neurotoxic effects of MDMA are generally believed to be increased when combined with amphetamine and other stimulants.
• MAOIs - This combination may increase the amount of neurotransmitters such as dopamine to dangerous or even fatal levels. Examples include syrian rue, banisteriopsis caapi, and some antidepressants.^[7]
• Cocaine - This combination may increase strain on the heart to dangerous levels.

• Brazil: Possession, production and sale is illegal as it is listed on Portaria SVS/MS nº 344.^[8]
• China: As of October 2015, pentedrone is a controlled substance in China.^[9]
• Czech Republic: Pentedrone is banned in the Czech Republic.^[10]
• Germany: Pentedrone is controlled under Anlage II BtMG (Narcotics Act, Schedule II)^[11] as of July 17, 2013.^[12] It is illegal to manufacture, possess, import, export, buy, sell, procure or dispense it without a license.^[13]
• Switzerland: Pentedrone is a controlled substance specifically named under Verzeichnis D.^[14]
• Turkey: Pentedrone is a classed as drug and is illegal to possess, produce, supply, or import.^[15]
• The Netherlands: Pentedrone is currently legal, but it is part of a substance group that may be banned soon as part of a recently passed law on New Psychoactive Substances (NPS). ^[16]
• United Kingdom: Pentedrone is a Class B drug in the United Kingdom as a result of the cathinone catch-all clause.^[17]
• United States: On January 28, 2014, the DEA listed it, along with 9 other synthetic cathinones, on the Schedule 1 with a temporary ban, effective February 27, 2014.^[18]

• Responsible use
• Designer drug
• Psychoactive substance index
• Stimulant
• Substituted cathinone
• N-Ethylpentedrone (NEP)
• Hexedrone
• MDPV

• Pentedrone (Wikipedia)
• Pentedrone (Isomer Design)
• Pentedrone (Forum)

• Simmler, L. D., Rickli, A., Hoener, M. C., & Liechti, M. E. (2014). Neuropharmacology Monoamine transporter and receptor interaction profiles of a new series of designer cathinones. Neuropharmacology, 79, 152–160. https://doi.org/10.1016/j.neuropharm.2013.11.008
• Hwang, J., Kim, J., Oh, J., Hong, S., Ma, S., Jung, Y., … Jang, C. (2014). The new stimulant designer compound pentedrone exhibits rewarding properties and affects dopaminergic activity, 117–128. https://doi.org/10.1111/adb.12299