Methylone Stats & Data
CNC(C)C(=O)c1ccc2OCOc2c1VKEQBMCRQDSRET-UHFFFAOYSA-NInteraction Warnings
Methylone can be potentially dangerous in combination with other stimulants as it can increase one's heart rate and blood pressure to dangerous levels.
This combination may increase strain on the heart.
Pharmacology
DrugBankMechanism of Action
A reproducible, simple, and small-scale method for determining the re-uptake and release of monoamines (dopamine, serotonin (5-HT) and norepinephrine) using rat brain synaptosomes /was developed/. These assays were then applied to study the effects of different kinds of non-medically used psychoactive drugs on monoamine re-uptake and release. The phenethylamine derivatives, 4-fluoroamphetamine, 2-methylamino-3,4-methylene-dioxy-propiophenone (methylone), 1-(1,3-benzodioxol-5-yl)-2-butanamine (BD
Metabolism
In recent years, a new class of designer drugs has appeared on the drugs of abuse market in many countries, namely, the so-called beta-keto (bk) designer drugs such as mephedrone (bk-4-methylmethamphetamine), butylone (bk-MBDB), and methylone (bk-MDMA). The aim of the present study was to identify the metabolites of mephedrone in rat and human urine using GC-MS techniques and to include mephedrone, butylone, and methylone within the authors' systematic toxicological analysis (STA) procedure. Six
Receptor Profile
Receptor Actions
History & Culture
1996–present
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. The synthesis occurred after the publication of Shulgin's PiHKAL in 1991, and consequently methylone was not included in that work; it was later documented in The Shulgin Index (2011). Jacob and Shulgin patented methylone as a potential antidepressant and antiparkinsonian agent, though these therapeutic applications were never developed or brought to market. Shulgin himself noted that the compound has "almost the same potency of MDMA, but it does not produce the same effects," describing it as having "an almost antidepressant action, pleasant and positive, but not the unique magic of MDMA." The name "methylone" later created some confusion, as it is also a trademarked brand name for an injectable form of methylprednisolone, a corticosteroid hormone used to treat arthritis and severe allergic reactions. While an alternate chemical nomenclature of bk-MDMA (beta-keto-MDMA) was proposed, "methylone" had already become widely established before the trademark conflict was noticed. The analogous naming convention was however adopted for related compounds such as bk-MDEA and bk-MBDB.
2004–2006
Methylone was encountered as a designer and recreational drug by 2004, approximately a decade after its initial synthesis. The compound was marketed under various product names, most notably "Explosion," which was confirmed through chemical analysis to contain methylone as its active ingredient. It was also sold as pure powder and in formulations marketed as household chemicals. In the Netherlands, methylone was available in smartshops until early April 2005. In New Zealand, the substance was sold from November 2005 to April 2006 as an MDMA substitute under the brand name "Ease," before being withdrawn following legal disputes with the government. During its period of legal availability, methylone was frequently mis-sold as MDMA. However, users have characterized it as less empathogenic and more stimulating than MDMA, with a notably shorter duration of effects.
2024–present
Despite never being developed following its original 1996 patent for antidepressant and antiparkinsonian use, methylone has re-emerged as a subject of clinical investigation. Under the developmental code TSND-201, Transcend Therapeutics is investigating the compound for the treatment of post-traumatic stress disorder (PTSD). As of July 2024, the substance is in phase 2 clinical trials for this indication.
Subjective Effect Notes
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.
Effect Profile
Curated + 228 ReportsStrong empathy, stimulation, sensory enhancement, and euphoria
Strong stimulation, anxiety/jitters, and euphoria with moderate focus
Empirical Duration
Erowid ReportsCommunity Effects
TripSitTolerance & Pharmacokinetics
drugs.wikiTolerance Decay
Cross-Tolerances
Demographics
Gender Distribution
Age Distribution
Reports Over Time
Effect Analysis
Erowid + BluelightEffects aggregated from 217 experience reports (167 Erowid + 61 Bluelight)
Effect Sentiment Distribution
Confidence Distribution
Positive Effects 63
Adverse Effects 59
Dose-Response Correlation
How effect frequency changes across dose levels
View data table
| Effect | Light (n=32) | Common (n=48) | Strong (n=10) |
|---|---|---|---|
| Euphoria | 75.0% | 77.1% | 70.0% |
| Empathy | 53.1% | 64.6% | 50.0% |
| Stimulation | 62.5% | 60.4% | 40.0% |
| Music Enhancement | 59.4% | 56.2% | 50.0% |
| Anxiety | 46.9% | 45.8% | 20.0% |
| Tactile Enhancement | 40.6% | 37.5% | 20.0% |
| Visual Distortions | 40.6% | 35.4% | 40.0% |
| Nausea | 28.1% | 22.9% | 40.0% |
| Body High | 28.1% | 22.9% | 40.0% |
| Jaw Clenching | 37.5% | 25.0% | 30.0% |
| Sedation | 31.2% | 37.5% | 30.0% |
| Color Enhancement | 21.9% | 27.1% | 30.0% |
| Auditory Effects | 15.6% | 8.3% | 30.0% |
| Pupil Dilation | 28.1% | 14.6% | 0% |
| Focus Enhancement | 28.1% | 22.9% | 0% |
Subjective Effect Ontology
Experience ReportsStructured effect tags extracted from 228 Erowid & Bluelight experience reports using a controlled vocabulary of 220+ canonical effects across 15 domains.
Emotional
Motor
Dose–Effect Mapping
Experience ReportsHow reported effects shift across dose tiers, based on 167 experience reports.
| Effect | Light (n=32) | Common (n=48) | Strong (n=10) | |
|---|---|---|---|---|
| euphoria | → | |||
| empathy | → | |||
| stimulation | ↓ | |||
| music enhancement | ↓ | |||
| anxiety | ↓ | |||
| tactile enhancement | ↓ | |||
| visual distortions | → | |||
| nausea | ↑ | |||
| body high | ↑ | |||
| jaw clenching | ↓ | |||
| sedation | → | |||
| color enhancement | ↑ | |||
| auditory effects | ↑ | |||
| pupil dilation | — | ↓ | ||
| focus enhancement | — | ↓ | ||
| increased heart rate | — | → | ||
| introspection | ↑ | |||
| muscle tension | ↓ | |||
| confusion | — | → | ||
| sweating | → |
Showing top 20 of 30 effects
Risk Escalation
Sentiment AnalysisAverage frequency of positive vs adverse effects across dose tiers
View effect breakdown
Adverse Effects
| Effect | Light (n=32) | Common (n=48) | Strong (n=10) | Change |
|---|---|---|---|---|
| Anxiety | -57% | |||
| Nausea | +42% | |||
| Jaw Clenching | -20% | |||
| Pupil Dilation | — | -48% | ||
| Increased Heart Rate | — | -3% | ||
| Muscle Tension | -20% | |||
| Confusion | — | +14% | ||
| Sweating | -8% | |||
| Memory Suppression | — | +222% | ||
| Headache | — | -34% | ||
| Appetite Suppression | — | — | 0% | |
| Motor Impairment | — | — | 0% |
Positive Effects
| Effect | Light (n=32) | Common (n=48) | Strong (n=10) | Change |
|---|---|---|---|---|
| Euphoria | -6% | |||
| Empathy | -5% | |||
| Stimulation | -36% | |||
| Music Enhancement | -15% | |||
| Tactile Enhancement | -50% | |||
| Body High | +42% | |||
| Color Enhancement | +36% | |||
| Focus Enhancement | — | -18% | ||
| Introspection | +28% | |||
| Creativity Enhancement | — | -32% | ||
| Pain Relief | — | — | 0% |
Dosage Distribution
Dose distribution from experience reports
Oral
Insufflated
Real-World Dose Distribution
62K DosesFrom 294 individual dose entries
Oral (n=213)
Insufflated (n=46)
Intravenous (n=11)
Common Combinations
Most co-occurring substances in experience reports
Form / Preparation
Most common forms and preparations reported
Body-Weight Dosing
Dose relative to body weight from reports with weight data
Oral
Insufflated
Redose Patterns
Redosing behavior across 133 reports
Legal Status
| Country | Status | Notes |
|---|---|---|
| Austria | Illegal (SMG) | Prohibited under the Suchtmittelgesetz (Narcotics Act) since June 26, 2019. Possession, production, and sale are illegal. |
| Brazil | Controlled | Listed as a controlled substance under Portaria SVS/MS nº 344. Added to national controls on February 18, 2014, alongside several other synthetic cathinones and phenethylamines. |
| Canada | Unclear/Possibly unscheduled | Not explicitly listed on the schedules of the Controlled Drugs and Substances Act. Health Canada has suggested it may fall under amphetamine analogue provisions; however, methylone bears the same chemical distinction from amphetamine as cathinone does, and cathinone is specifically not considered an amphetamine analogue, creating legal ambiguity. |
| Croatia | Controlled | Reportedly outlawed in February 2011 under national drug control legislation. |
| Denmark | Controlled | Illegal since February 8, 2008, with exceptions permitted only for scientific and medicinal research purposes. |
| Estonia | Schedule I | Added to Schedule I in February 2011 alongside several other cathinone derivatives and synthetic cannabinoids. |
| Finland | Controlled (hard-drug category) | Listed on the Finnish controlled substances schedule in the hard-drug category, carrying penalties associated with serious drug offenses. |
| Germany | Anlage II BtMG | Listed under Anlage II of the Betäubungsmittelgesetz (Narcotics Act) as of July 2012. Manufacturing, possession, import, export, purchase, sale, procurement, and dispensing without a license is illegal. |
| Netherlands | Medicine Act (unregistered) | Covered under the Medicine Act (Geneesmiddelenwet). Since methylone is not officially registered as an approved pharmaceutical, trading in the substance is prohibited. Previously available in smartshops until April 2005 when the Public Health Minister declared it illegal. |
| New Zealand | Class C (by interpretation) | Not explicitly scheduled under the Misuse of Drugs Act and falls outside the strict definition of an 'amphetamine analogue,' but law enforcement authorities consider it 'substantially similar' to methcathinone and treat it as a Class C controlled substance. |
| Russia | Schedule I | Classified as a Schedule I prohibited substance under Russian drug control legislation. |
| Slovak Republic | Controlled | Controlled substance as of March 1, 2011, scheduled alongside other synthetic cathinones and cannabinoid receptor agonists. |
| Sweden | Schedule I | Classified as a Schedule I narcotic substance as of October 1, 2010. |
| Switzerland | Controlled (Verzeichnis D) | Specifically named as a controlled substance under Verzeichnis D of Swiss narcotics legislation. |
| United Kingdom | Class B | Controlled under the Misuse of Drugs Act 1971 as part of the cathinone catch-all clause. Import and sale restrictions took effect March 31, 2010, with full controls enacted April 16, 2010. |
| United States | Schedule I | The DEA issued an emergency scheduling order on October 21, 2011, followed by a final rule permanently adding methylone to Schedule I on April 12, 2013. Manufacturing, possession, and distribution without a DEA license is prohibited. Prior to federal action, numerous states including Florida, Louisiana, Georgia, and Pennsylvania enacted their own emergency bans on methylone as part of 'bath salts' legislation beginning in early 2011. |
References
Data Sources
Cited References
- Bluelight: The Big & Dandy bk-MDMA (Methylone) Thread
- Cozzi et al. 1999 - Inhibition of plasma membrane monoamine transporters by beta-ketoamphetamines
- Erowid Methylone Vault: Dosage
- Erowid Methylone Vault: Effects
- Nagai et al. 2007 - The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain
- Poyatos et al. 2022 - Pharmacological effects of methylone and MDMA in humans
- TripSit Wiki: Drug Combinations
- TripSit Factsheet: Methylone