Methylone
Methylone is a synthetic stimulant and entactogen of the cathinone class. First synthesized by Peyton Jacob III and Alexander Shulgin in 1996 as a potential antidepressant,citation needed it later gained popularity as a recreational substance.1 Methylone is frequently used as a substitute for MDMA due to overlapping effects,citation needed though Shulgin himself described it as lacking MDMA's "unique magic," noting it is more stimulating and less empathogenic. It has been commonly mis-sold as MDMA.
Dosage & Duration
Dosage
Doses are population estimates that vary widely between individuals.
Redosing may not reliably intensify or prolong effects. Maintain adequate hydration throughout the experience.
Duration
Subjective Effects
Legacy content. A statistically backed ontology from Mindstate Design Labs is coming soon.
Effects vary widely by individual, dose, and context.
Physical
Cognitive
The general head space of methylone is described by many as one of extreme mental stimulation, feelings of love or empathy and powerful euphoria. It contains a large number of typical psychedelic, entactogenic and stimulant cognitive effects.
Visual
Pharmacology
Pharmacodynamics
Methylone acts as a mixed releasing agent and reuptake inhibitor of serotonin, norepinephrine, and dopamine.2 Its serotonin transporter affinity (Ki of 242.1 nM) is roughly 3-fold lower than that of MDMA, while its norepinephrine and dopamine transporter affinities are comparable; its VMAT2 affinity is approximately 13-fold lower, contributing to a profile that balances reuptake inhibition with monoamine release rather than acting as a predominant releaser.citation needed Methylone is also a variable-potency partial agonist at 5-HT1A, 5-HT1B, and 5-HT1D receptors and shows no significant activity at 5-HT2A or 5-HT2B receptors. Its activity at 5-HT2C is uncertain, with one study reporting no significant affinity and another finding potent near-full agonism via the Gαq signaling pathway.
Pharmacokinetics
In humans, the mean elimination half-life of methylone following oral doses of 50 to 200 mg ranges from 5.8 to 6.9 hours.citation needed The two major metabolic pathways are N-demethylation to methylenedioxycathinone (MDC) and demethylation followed by O-methylation, producing 4-hydroxy-3-methoxymethcathinone (HMMC) and 3-hydroxy-4-methoxymethcathinone (3-OH-4-MeO-MC). An additional metabolite, 3,4-dihydroxymethcathinone (HHMC), has also been identified. In rats administered 5 mg/kg, approximately 26% was excreted as HMMC within 48 hours, with less than 3% excreted unchanged.
Dangerous
Highest riskThese combinations are considered extremely harmful and should always be avoided. Reactions to these drugs taken in combination are highly unpredictable and have a potential to cause death.
Tolerance
Tolerance timelines are rules of thumb, not exact schedules, and vary widely between individuals and use patterns.
Dopaminergic stimulants
Harm Potential
Addiction & Dependence
Psychological
ModerateChronic use of methylone can be considered moderately addictive with a high potential for abuse and is capable of causing psychological dependence among certain users.citation needed Compulsive redosing is commonly reported, likely promoted by the substance's time compression effects which speed up the subjective experience.
Physical
LowWhen addiction has developed, cravings and withdrawal effects may occur if a person suddenly stops their usage. The nature and severity of withdrawal symptoms have not been well characterized.
Toxicity
Higher doses and repeated use have been associated with chest pains, heart palpitations, and elevated blood pressure and heart rate; worrying cardiovascular increases have been reported at doses exceeding 180-200 mg.citation needed
Temperature regulation suppression and increased body temperature occur during use, with hyperthermia risk elevated during physical activity in hot environments such as dance venues.citation needed
Psychosis Risk
Abuse at high dosages for prolonged periods can potentially result in stimulant psychosis presenting with paranoia, hallucinations, or delusions. Based on research into similar stimulants, approximately 5-15% of those who develop stimulant psychosis may not recover completely,citation needed though antipsychotic medications effectively resolve symptoms of acute psychosis. Psychosis very rarely arises from occasional or moderate use.
Seizure Risk
Limited data on seizure risk from methylone use alone.
History & Culture
Discovery and Development
Methylone was first synthesized by chemists Peyton Jacob III and Alexander Shulgin in the mid-1990s, with the compound first described in scientific literature by 1996.citation needed The synthesis occurred after the publication of Shulgin's PiHKAL in 1991, and consequently methylone was not…
Legality
International
Methylone is listed in Schedule II of the Convention on Psychotropic Substances of 1971. It is not listed under the 1961 Single Convention on Narcotic Drugs or the 1988 Convention against Illicit Traffic in Narcotic Drugs and Psychotropic Substances.
By Country
References
Source Pages
Bluelight: The Big & Dandy bk-MDMA (Methylone) Thread
Disregard Everything I Say
Drug Users Bible by Dominic Milton Trott
Erowid
Erowid Methylone Vault: Dosage
Erowid Methylone Vault: Effects
Isomer Design (TiHKAL/PiHKAL)
PsychonautWiki
TripSit Factsheet: Methylone
TripSit Factsheets
TripSit Wiki: Drug Combinations
Wikipedia
Citations
- Poyatos L, Pérez-Mañá C, Hladun O, & et al.. (2023). Pharmacological effects of methylone and MDMA in humans. 14. https://doi.org/10.3389/fphar.2023.11228611
- The designer methcathinone analogs, mephedrone and methylone, are substrates for monoamine transporters in brain tissue. Neuropsychopharmacology, 37(5), 1192–1203 (2012). https://doi.org/10.1038/npp.2011.3041
- Gloria Daziani, Alfredo Fabrizio Lo Faro, Vincenzo Montana, Gaia Goteri, Mauro Pesaresi, Giulia Bambagiotti, Eva Montanari, Raffaele Giorgetti, & Angelo Montana. (March 2023). Synthetic Cathinones and Neurotoxicity Risks: A Systematic Review. Int J Mol Sci, 24(7), 6230. https://doi.org/10.3390/ijms240762301
- Raúl López-Arnau, Jordi Camarasa, Marcel·lí Carbó, Núria Nadal-Gratacós, Pol Puigseslloses, María Espinosa-Velasco, Edurne Urquizu, Elena Escubedo, & David Pubill. (2022). 3,4-Methylenedioxy methamphetamine, synthetic cathinones and psychedelics: From recreational to novel psychotherapeutic drugs. Front Psychiatry, 13. https://doi.org/10.3389/fpsyt.2022.9904051
- Amanda Jones, Jennifer Warner-Schmidt, Hannah Kwak, Martin Stogniew, Blake Mandell, Terence H.W. Ching, Murray B. Stein, & Benjamin Kelmendi. (February 2026). Efficacy and Safety of the Neuroplastogen TSND-201 for the Treatment of PTSD: A Randomized Clinical Trial. JAMA Psychiatry. https://doi.org/10.1001/jamapsychiatry.2025.462512
- Decreto 122/2026, Anexo I del Decreto 560/2019. argentina.gob.ar (n.d.). https://www.argentina.gob.ar/normativa/nacional/norma-423520/texto1
- Decreto 122/2026, Anexo I del Decreto 560/2019. argentina.gob.ar (n.d.). https://www.argentina.gob.ar/normativa/nacional/decreto-560-2019-326675/actualizacion1
- Decreto 122/2026, Anexo I del Decreto 560/2019. argentina.gob.ar (n.d.). https://www.argentina.gob.ar/normativa/nacional/ley-23737-138/actualizacion1
- Therapeutic Goods (Poisons Standard—June 2026) Instrument 2026, Schedule 9. legislation.gov.au (n.d.). https://www.legislation.gov.au/F2026L00633/latest/text1
- Therapeutic Goods (Poisons Standard—June 2026) Instrument 2026, Schedule 9. legislation.gov.au (n.d.). https://www.legislation.gov.au/F2026L00633/latest/details1
Article Status
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Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
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