Methylone

1-(1,3-benzodioxol-5-yl)-2-(methylamino)propan-1-one

Overview

Methylone belongs to Entactogens/Empathogens / Cathinones.

Key safety note: Methylone is a synthetic cathinone (a β-keto MDMA analogue) sold as a 'bath salts'/'research chemical' powder or crystal, often mis-sold as or cut into 'ecstasy'/MDMA.[4][5]
Effects
Subjective effects vary. What a substance feels like depends on dose, individual physiology, mindset, and setting. The points below describe commonly reported effects, not guaranteed, uniform, or desirable outcomes.
  • Euphoria, emotional warmth, empathy and sociability with stimulation, increased energy and talkativeness: an MDMA-like entactogenic effect but generally milder, more stimulant and shorter-lived, with less of MDMA's depth of empathy.
  • Sympathetic effects: raised heart rate and blood pressure, dilated pupils, jaw clenching/teeth grinding, sweating, raised body temperature and reduced appetite.
  • The brief, less-satisfying reward encourages compulsive redosing. Comedowns bring anxiety, low mood, irritability, insomnia, cognitive fatigue and craving, and can last well into the next day.
Dosing & duration
Harm-reduction note: These are commonly cited reference ranges, not a recommendation or a “safe” dose. Potency, purity, body chemistry, tolerance, and drug combinations vary widely. Start low, go slow, wait for full effects before redosing, and never assume an unknown product matches these figures. Missing data is not evidence of safety.

Oral (swallowed) or insufflated. The values below are approximate ORAL figures.. Not a recommendation. Methylone is short-acting and reinforcing, which drives compulsive redosing and binges: the biggest source of harm. Insufflated doses are lower and faster in onset but harsher and shorter. Use a milligram scale, start low, space out or avoid redosing, keep cool and hydrated (but not excessively), and never combine with other stimulants or serotonergic drugs. Grey-market powders are frequently mis-sold or cut: test the substance.

Dose ranges

Threshold

75 mg

Light

75–150 mg

Common

150–225 mg

Strong

225–325 mg

Heavy

325 mg +

Duration

onset

15–45 min (oral)

total

2.5–4 h (oral)

after effects

6–24 h (anxiety, low mood, fatigue, craving)

Chemical & Physical Properties
FormulaC11H13NO3
Molar mass207.23 g/mol
StateSolid (usually the hydrochloride salt, white to off-white crystalline powder or crystals)
Melting pointNot reported
Boiling pointNot reported
DensityNot reported
Vapor pressureNot reported
pKaNot reported
LogP0.6 (predicted, XLogP3, free base)
SolubilityNot reported
Refractive indexNot reported
Identifiers & Synonyms
CAS186028-79-5
CAS (enantiomer)
PubChem CID45789647
InChIKeyVKEQBMCRQDSRET-UHFFFAOYSA-N
InChIInChI=1S/C11H13NO3/c1-7(12-2)11(13)8-3-4-9-10(5-8)15-6-14-9/h3-5,7,12H,6H2,1-2H3
SMILESCC(C(=O)C1=CC2=C(C=C1)OCO2)NC

Synonyms

  • 3,4-Methylenedioxy-N-methylcathinone
  • βk-MDMA
  • MDMC
  • M1
  • Explosion
Pharmacodynamics & Biochemistry

Methylone (3,4-methylenedioxy-N-methylcathinone, βk-MDMA) is the β-keto ('cathinone') analogue of MDMA: MDMA with a ketone on the β-carbon of the side chain. Like MDMA it is a non-selective, substrate-type releaser at the dopamine (DAT), noradrenaline (NET) and serotonin (SERT) transporters, and a much weaker reuptake inhibitor, giving it a mixed stimulant–entactogen profile. It is broadly MDMA-like but somewhat less potent, with a relatively larger dopaminergic contribution and weaker serotonin release, which is thought to underlie its more stimulant and less profoundly empathogenic character. It has essentially no affinity for the 5-HT2A/5-HT2C receptors and is inactive at TAAR1, and it is a considerably weaker substrate for the vesicular monoamine transporter VMAT2 than MDMA (~13-fold), a difference that may shape its serotonergic/neurotoxic profile. In rat brain synaptosomes methylone behaves as a monoamine-releasing agent with release EC50 values of ~133 nM (DAT), ~152 nM (NET) and ~242 nM (SERT): a non-selective releaser of MDMA-like potency and balance. In transfected human (HEK293) cells it inhibits monoamine uptake far more weakly and with a dopamine-over-serotonin bias: IC50 ≈ 0.54 µM (NET), 4.8 µM (DAT) and 15.5 µM (SERT): consistent with a compound that primarily carries monoamines out of the nerve terminal (a releaser) rather than simply blocking their reuptake. Its faster onset and shorter duration than MDMA tend to promote compulsive redosing.

Biological targets

  • DAT
  • NET
  • SERT

Binding & functional measurements

TargetMeasurementSpecies
Dopamine transporterKi 2,730 ± 200 nMHuman
Pharmacokinetics
BioavailabilityOral or insufflated, rapid onset
TmaxNot reported
Half-lifeReported elimination half-life on the order of a few hours (≈2–7 h across studies), subjective effects are shorter (≈2.5–4 h), which encourages redosing
VdNot reported
Protein bindingNot reported
MetabolismHepatic: N-demethylation to methylenedioxycathinone (MDC), and O-demethylenation of the methylenedioxy ring followed by O-methylation (COMT) to hydroxy-methoxy metabolites. CYP enzymes implicated include CYP2D6, CYP2B6, CYP1A2 and CYP2C19
ExcretionRenal
Toxicology & Safety
Harm-reduction note: Toxicity and risk depend on dose, route, purity, combinations, setting, and individual health factors. Missing harms should never be interpreted as evidence of safety.

Not reported

Methylone is a synthetic cathinone (a β-keto MDMA analogue) sold as a 'bath salts'/'research chemical' powder or crystal, often mis-sold as or cut into 'ecstasy'/MDMA. Its shorter, less euphoric effect than MDMA encourages compulsive redosing and binges, which are the main source of harm. Acute risks are those of a serotonergic stimulant: tachycardia, hypertension, palpitations and cardiovascular strain, hyperthermia (worsened by hot, crowded settings and dehydration), sweating, teeth-grinding, dilated pupils, anxiety, agitation and, at high doses or in binges, stimulant psychosis, seizures and serotonin toxicity. It carries a real serotonin-syndrome risk when combined with MAOIs, SSRIs/SNRIs or other serotonergic drugs, and deaths have occurred, frequently with co-used alcohol or other stimulants. Because identity and strength of grey-market powders vary widely, test the substance, use a milligram scale, start low, avoid or space out redosing, keep cool and hydrated (but do not over-drink water), and never combine with other stimulants or serotonergic medication.[4][5]

Legal Status
Legal note: Legal status can change over time and may vary by country, region, formulation, analogue status, prescription context, and enforcement practice. Always confirm with current official sources before relying on this section.
Interactions & Contraindications

Drug interactions

MAOIs Serotonin syndrome risk.[4]
SSRIs, SNRIs, Other serotonergic drugs Serotonin syndrome risk (SSRIs/SNRIs, other releasers such as MDMA).[4]
Stimulants (amphetamines, cocaine) Additive cardiovascular strain and hyperthermia (cocaine, amphetamines, other cathinones).[4]
Alcohol Depressants mask the stimulation and encourage overuse, alcohol co-use features in many cathinone-related deaths.[4][5]

Contraindications

Cardiovascular disease, hypertension or arrhythmia hypertension or arrhythmia.[4]
Personal or family history of psychosis, schizophrenia or bipolar disorder or severe anxiety.[4]
Concurrent MAOI, SSRI/SNRI or other serotonergic medication concurrent MAOIs or SSRIs, or other stimulants.[4]
Hot, dehydrating environments (overheating risk) hot, dehydrating settings.[4]
Pregnancy or breastfeeding
Usage & Context
  • A recreational stimulant–entactogen used for MDMA- and amphetamine-like euphoria, stimulation, warmth and sociability: usually swallowed or insufflated as a powder/crystal. It is frequently encountered mis-sold as or adulterating 'ecstasy'.
  • First patented in 1996 (by Peyton Jacob III and Alexander Shulgin as a potential antidepressant), it re-emerged in the late 2000s as one of the earliest and most widespread 'bath salts'/'legal high' synthetic cathinones, its spread helping drive new-psychoactive-substance legislation.
  • It has no accepted medical use and is now controlled in most jurisdictions (US Schedule I, UK Class B, DE Anlage II BtMG).
Sources & Evidence

Further Information