|Summary sheet: 4F-MPH|
|Systematic name||Methyl 2-(4-fluorophenyl)-2-(piperidin-2-yl)acetate|
|Chemical class||Phenidate / Piperidine|
|Routes of Administration|
4-Fluoromethylphenidate (commonly known as 4F-MPH) is a novel synthetic stimulant of the substituted phenethylamine and piperidine classes that produces long-lasting euphoriant, and stimulating effects when administered. It is a closely related structural analog of the commonly prescribed ADHD drug methylphenidate (known by the brand-names Ritalin and Concerta).
The two substances are believed to have very similar pharmacological mechanisms as monoamine reuptake inhibitors but have been reported to display distinctive subjective effects, with 4F-MPH being considered significantly more euphoric and recreational. Anecdotal reports suggest that it is considerably more potent with fewer uncomfortable side effects such as anxiety, muscle spasms and compulsive redosing. This perhaps owes to the fact that it has been shown to act as a higher efficiency dopamine reuptake inhibitor than the parent compound methylphenidate.
4F-MPH has an extremely short history of recreational use and has yet to be documented being sold on the streets. It was initially developed as a replacement for ethylphenidate which became illegal in the United Kingdom on April 2015 following a temporary blanket ban. Shortly after, it recently became made available for sale on the online gray market as a research chemical for global distribution.
Due to its potent, long-lasting stimulant effect, likely habit-forming properties as well as unknown toxicity profile, it is strongly recommended that one use proper harm reduction practices if choosing to use this substance.
4F-MPH is a synthetic molecule of the substituted phenethylamine and piperidine classes, and a fluorinated analog of methylphenidate. It contains a phenethylamine core featuring a phenyl ring bound to an amino -NH2 group through an ethyl chain. It is structurally similar to amphetamine, featuring a substitution at Rα which is incorporated into a piperidine ring ending at the terminal amine of the phenethylamine chain. Additionally, it contains a methyl acetate bound to R2 or its structure. 4F-MPH is structurally identical to methylphenidate with the exception of a single fluorine atom bound to the four position on the phenethylamine core.
With respect to nomenclature, the methyl- in methylphenidate regards the side chain of one carbon atom, while phen- indicates the phenyl ring. Id- is contracted from a piperidine ring, and -ate indicates the acetate group containing the oxygen atoms. Like its parent molecule, 4F-MPH is a chiral compound, presumably produced as a racemic mixture.
Of note is the scientific finding that amphetamine analogs containing fluorine, chlorine, bromine and methyl groups are typically stronger than those without.
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4F-MPH is thought to act primarily as a dopamine reuptake inhibitor, meaning it effectively boosts the levels of dopamine neurotransmitters in the brain by binding to and partially blocking the transporter proteins that normally clear these monoamines from the synaptic cleft. This allows dopamine to accumulate within the reward pathways in the brain, resulting in stimulating and euphoric effects.
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The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances and are more likely to induce a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.
- 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:
Many users of this compound have reported positive, functional cognitive effects associated with the therapeutic aspect of traditional stimulants. This may owe to its similarities to methylphenidate, in which these effects have been well-studied.
- Analysis enhancement
- Euphoria - The euphoric rush associated with 4F-MPH use (as result of dopamine reuptake inhibition) is very short-lived and compulsive, similar to that of cocaine.
- Cognitive fatigue - This component can occur during the offset of this compound as a rebound effect which is usually equal in its intensity to the enhancements which occurred before it.
- Emotion suppression - This component has been reported as being more prominent than with other stimulants, and is in-line with the noted emotion-suppressing effects that have been observed with other stimulants, but particularly methylphenidate and related compounds.
- Focus enhancement - This component is most effective at low to moderate dosages as anything higher will usually impair concentration.
- Increased music appreciation
- Motivation enhancement
- Thought acceleration
- Thought organization - This component has been reported as being more prominent than with other stimulants, which has led some users to adopt it for productive or functional purposes rather than hedonic ones.
Toxicity and harm potential
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The toxicity and long-term health effects of recreational 4F-MPH use do not seem to have been studied in any scientific context and the exact toxic dosage is unknown. This is because 4F-MPH is a research chemical with very little history of human usage. Anecdotal evidence from people who have tried 4F-MPH suggests that there are no negative health effects attributed to simply trying the drug by itself at low to moderate doses and using it very sparingly (but nothing can be completely guaranteed). Independent researchshould always be done to ensure that a combination of two or more substances is safe before consumption.
It is strongly recommended that one use harm reduction practices when using this drug.
Tolerance and addiction potential
In terms of its tolerance, 4F-MPH can be used multiple days in a row for extended periods of time, but acute tolerance does exist and builds up gradually over repeated extended use. This results in the user requiring an increase in dosage to achieve the same effects.
Although many psychoactive substances are safe to use on their own, they can become dangerous or even life-threatening when taken with other substances. The list below contains some potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses but still increase the possibility of injury of death. Independent research should always be conducted to ensure that a combination of two or more substances is safe before consumption.
- 25x-NBOMe - Members of the 25x-NBOMe family are very stimulating and should not be combined with stimulants due to the risk of excessive stimulation. This can result in panic attacks, thought loops, seizures, increased blood pressure, vasoconstriction, and heart failure in extreme cases.
- Alcohol - Alcohol can be dangerous to combine with stimulants due to the risk of accidental over-intoxication. Stimulants mask the sedative effects of alcohol, which is the main factor people use to assess their degree of intoxication. Once the stimulant wears off, the depressant effects of alcohol are left unopposed, which can result in blackouts and respiratory depression. If combined, one should strictly limit themselves to only drinking a certain amount of alcohol per hour.
- DXM - DXM should not be combined with stimulants due to its effects on serotonin and dopamine reuptake. This can lead to panic attacks, hypertensive crisis, or serotonin syndrome.
- MXE - Combining stimulants with MXE may dangerously elevate blood pressure and increase the risk of psychosis.
- Tramadol - Combining stimulants with tramadol increases the risk of seizures.
- MAOIs - This combination may increase the amount of neurotransmitters such as dopamine to dangerous or even fatal levels. Examples include syrian rue, banisteriopsis caapi, 2C-T-2, 2C-T-7, αMT, and some antidepressants.
- MDMA - The neurotoxic effects of MDMA may be increased when combined with other stimulants.
- Cocaine - This combination may unpredictably increase strain on the heart to a dangerous degree.
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- United Kingdom - 4-Fluoromethylphenidate is a class B drug in the UK as of 31st May 2017 and is illegal to possess, produce or supply. 
- United States: 4-Fluromethylphenidate is a Schedule I controlled substance in the state of Alabama.
- Deutsch, H. M., Shi, Q., Gruszecka-Kowalik, E., & Schweri, M. M. (1996). Synthesis and pharmacology of potential cocaine antagonists. 2. Structure-activity relationship studies of aromatic ring-substituted methylphenidate analogs. Journal of medicinal chemistry, 39(6), 1201-1209. https://www.doi.org/10.1021/jm950697c
- Biochemical and behavioral characterization of novel methylphenidate analogs (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/11961053
- Synthesis of methylphenidate analogues and their binding affinities at dopamine and serotonin transport sites (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/15026075
- Quantitative structure-activity relationship studies of threo-methylphenidate analogs (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/20846865
- Chemistry, Design, and Structure−Activity Relationship of Cocaine Antagonists | http://pubs.acs.org/doi/abs/10.1021/cr9700538
- Gillman, P. K. (2005). Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity. British Journal of Anaesthesia, 95(4), 434-441. https://doi.org/10.1093/bja/aei210
- The Misuse of Drugs Act 1971 (Amendment) Order 2017 (Legislation.gov.uk) | http://www.legislation.gov.uk/uksi/2017/634/made
- Controlled substances, Schedule I, additional synthetic controlled substances and analogue substances included in, trafficking in controlled substance analogues, requisite weight increased, Secs. 13A-12-231, 20-2-23 am'd. | https://legiscan.com/AL/text/SB333/2014