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Butylone (also known as β-keto-N-methylbenzodioxolylbutanamine, βk-MBDB, or B1) is a synthetic entactogen and stimulant substance of the cathinone class. It is the β-keto analog of MBDB and the substituted methylenedioxy analogue of buphedrone.

As a designer drug, it is commonly sold on the street along with ethylone as a substitute or counterfeit for MDMA and methylone (all of which have collectively come to be referred to as "Molly") due to methylone's declining availability on the research chemical market. However, in spite of behavioral and pharmacological similarities between butylone and MDMA, the observed subjective effects of both substances are not completely identical.

Subjective Effects

Subjective effects include stimulation, thought acceleration, motivation enhancement, increased libido, appetite suppression, and euphoria. Butylone is reported to be less potent than its relatives methylone and ethylone as well as possessing more classic stimulant as opposed to entactogenic effects.

Butylone has a very short history of human use and very little data exists about its pharmacological properties, metabolism, and toxicity. It is highly advised to use harm reduction practices if using this substance.

Chemistry

Butylone, or β-keto-N-methylbenzodioxolylbutanamine, is a synthetic molecule of the cathinone family. Cathinones are structurally similar to amphetamines in that they contain a phenethylamine core featuring a phenyl ring bound to an amino (NH2) group through an ethyl chain with an additional ethyl substitution at Rα. Cathinones such as butylone are alpha-methylated phenethylamines (i.e. amphetamines) but differ from them with the addition of a ketone functional group (a carbonyl group at Rβ). Butylone contains a methyl substitution at RN, a substitution which is shared with MDEA, ethylone, 4-MEC, and certain other stimulants and entactogens. Additionally, butylone contains substitutions at R3 and R4 of the phenyl ring with oxygen groups. These oxygen groups are incorporated into a methylenedioxy ring through a methylene chain. Butylone shares this methylenedioxy ring with MDA, MDAI, and MDMA.

Pharmacology

Butylone acts as a mixed reuptake inhibitor/releasing agent of serotonin, norepinephrine, and dopamine. These are the neurotransmitters in charge of pleasure, reward, motivation, and focus. This is done by inhibiting the reuptake and reabsorption of the neurotransmitters after they have performed their function of transmitting a neural impulse, essentially allowing them to accumulate and be reused, causing physically stimulating and euphoric effects.

In comparison to methylone, it has approximately over 4x lower affinity for the norepinephrine transporter, while its affinity for the serotonin and dopamine transporters is similar. The results of these differences in pharmacology relative to MDMA is that butylone, like its close analog ethylone is less potent in terms of dose, has more balanced catecholaminergic effects relative to serotonergic, and behaves more like a reuptake inhibitor like methylphenidate than a releaser like amphetamine; however, butylone still has relatively robust releasing capabilities.

Effects

Physical Effects

Stimulation - Butylone is renowned for its stimulating and energetic qualities. This makes it a favored choice for events like festivals and raves, where users engage in activities such as running, climbing, and dancing. At higher doses, the stimulation becomes pronounced, leading to jaw clenching, bodily shakes, and uncontrollable vibrations, resulting in a notable loss of motor control.

Spontaneous Physical Sensations - Users often experience a profound euphoric tingling sensation throughout their entire body. This sensation becomes increasingly pleasurable with higher doses and maintains a consistent presence, reaching its zenith at the peak of the experience.

Vibrating Vision - At elevated doses, users may encounter rapid, spontaneous wiggling of the eyeballs, causing temporary blurriness and visual disorientation, a phenomenon known as nystagmus.

Dehydration - Dry mouth and dehydration are common side effects of butylone use. This is primarily due to the increased heart rate and the strong urge to participate in physically demanding activities. While it is crucial to avoid dehydration, some users have suffered from over-drinking and water intoxication. Hence, it is advisable for users to sip water cautiously without overindulging.

Difficulty Urinating - Higher doses of butylone may lead to temporary difficulty in urination. This effect is harmless and results from butylone's influence on the release of anti-diuretic hormone (ADH), which regulates urination. This can be alleviated by relaxation and by using a warm compress to promote blood flow to the genital area.

Temperature Regulation Suppression

Tactile Enhancement

Increased Heart Rate

Increased Perspiration

Increased Blood Pressure

Teeth Grinding - While butylone induces teeth grinding, it is generally less intense than the teeth grinding associated with MDMA.

Cognitive Effects

The cognitive effects of butylone become more pronounced with increasing doses. Butylone is associated with extreme mental stimulation, mild feelings of love and empathy, and moderate euphoria. These cognitive effects include:

Cognitive Euphoria - Users experience strong emotional euphoria and happiness, likely stemming from serotonin and dopamine release. In comparison to MDMA, it is more akin to the euphoria experienced with amphetamine and mephedrone.

Empathy, Love, and Sociability Enhancement - While distinct and powerful, the feelings of love and empathy induced by butylone are less forceful and more internal compared to MDMA. Users may experience feelings of love and empathy but may not feel the need to express them outwardly.

Time Distortion - Butylone frequently causes strong feelings of time compression, making time seem to pass quickly.

Thought Acceleration

Analysis Enhancement

Mindfulness

Increased Libido

Increased Music Appreciation

After Effects

The post-stimulant effects during the offset of butylone use often include negative and uncomfortable sensations, referred to as the "comedown." This is primarily due to neurotransmitter depletion and may encompass:

Anxiety

Cognitive Fatigue

Depression

Irritability

Motivation Suppression

Thought Deceleration

Wakefulness

Harm Potential

Scientific study of the long-term health effects and toxicity of recreational butylone use is limited. Because of its relatively low history of human usage, there is insufficient information on its exact toxic dosage. Anecdotal evidence from users suggests that low to moderate doses used sparingly do not result in strong adverse effects.

Addiction Potential

Butylone, like other stimulants, has the potential to be moderately addictive, leading to psychological dependence in some users. When addiction develops, cravings and withdrawal effects may surface upon discontinuation. Tolerance to the effects of butylone may develop with prolonged and repeated use, necessitating larger doses to achieve the same effects. Reduction of tolerance may take 3 to 7 days, with a return to baseline expected within 1 to 2 weeks in the absence of further consumption. Butylone exhibits cross-tolerance with all dopaminergic stimulants, meaning its use may reduce the effects of other stimulants.

Psychosis

Prolonged, high-dosage use of stimulants, including butylone, can potentially lead to stimulant psychosis. This condition may involve symptoms like paranoia, hallucinations, or delusions. Full recovery may not occur in 5-15% of cases, as reported in the context of amphetamine, dextroamphetamine, and methamphetamine abuse-induced psychosis. Treatment with antipsychotic medications has shown effectiveness in resolving symptoms of acute amphetamine psychosis.

Legal Status

Legal status of butylone varies by country:

• Austria: Illegal
• Brazil: Illegal
• Canada: Controlled as a Schedule I substance
• China: Controlled substance
• Finland: Controlled substance
• Germany: Controlled substance
• Israel: Controlled substance
• Japan: Controlled substance
• Norway: Controlled substance
• Poland: Controlled substance
• Sweden: Controlled substance
• Switzerland: Controlled substance
• United Kingdom: Class B drug
• United States: Unscheduled, though it may be considered illegal under analog laws, such as the Federal Analog Act.

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