Disregard Everything I Say

Dosage (oral):

Threshold : 60mg
Light : 100 - 150mg
Common : 150 - 250mg
Strong : 200 - 300mg

Duration (oral):

Total : 3 - 5 hours
Onset : 20 - 60 minutes
Peak : 60 - 90 minutes
Offset : 60 - 120 minutes
After effects : 1 - 6 hours

Methylone (also known as M1, 3,4-methylenedioxy-N-methylcathinone, MDMC and bk-MDMA) is an entactogen and stimulant of the phenethylamine, amphetamine and cathinone classes. It was first synthesized by chemists Peyton Jacob III and Alexander Shulgin in 1996 for potential use as an antidepressant.

This compound is often used as a substitute for MDMA due to its similar range of subjective effects. However, in spite of behavioral and pharmacological similarities between methylone and MDMA, the observed subjective effects of both drugs are not completely identical. Alexander Shulgin wrote of the former:

“Methylone has almost the same potency of MDMA, but it does not produce the same effects. It has an almost antidepressant action, pleasant and positive, but not the unique magic of MDMA.”

“Methylone” is also a trademarked brand name for an injectable form of methylprednisolone, a corticosteroid hormone used to treat arthritis and severe allergic reactions; hence, methylone may be confused with it.

In terms of its chemistry, 3,4-methylenedioxy-N-methylamphetamine is part of the phenethylamine, cathinone and amphetamine families. There is a methylenedioxy ring attached to carbons R3 and R4, as well as methyl chains at Rα and RN. Methylone is a close structural analog of MDMA, differing by the addition of a β-ketone group attached to the beta position of the amine chain.

In terms of its pharmacology, methylone acts as a mixed reuptake inhibitor/releasing agent of serotonin, norepinephrine, and dopamine. These are the neurotransmitters in charge of pleasure, 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 MDMA, it has approximately 3x lower affinity for the serotonin transporter, while its affinity for the norepinephrine and dopamine transporters is similar. Notably, methylone’s affinity for the vesicular monoamine transporter 2 (VMAT2) is about 13x lower than that of MDMA. The results of these differences in pharmacology relative to MDMA are that methylone 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, methylone still has relatively robust releasing capabilities.

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely if ever occur all at once but heavier dosages will increase the chances and are more likely to induce a full range of effects.

Physical effects:

The physical effects of methylone can be broken down into seven components all of which progressively intensify proportional to dosage. These are described below and generally include:

• Spontaneous tactile sensations - The “body high” of methylone can be described as a moderate to extreme euphoric tingling sensation that encompasses the entire body. It is capable of becoming overwhelmingly pleasurable at higher dosages. This sensation maintains a consistent presence that steadily rises with the onset and hits its limit once the peak has been reached.
• Stimulation - In terms of its effects on the user’s physical energy levels, methylone is commonly considered to be extremely stimulating and energetic. This encourages activities such as running, climbing and dancing in a way that makes methylone a popular choice for musical events such as festivals and raves. The particular style of stimulation which methylone presents can be described as forced. This means that at higher dosages, it becomes difficult or impossible to keep still as jaw clenching, involuntarily bodily shakes, and vibrations become present, resulting in an extreme unsteadiness of the hands and a general lack of motor control.
• Vibrating vision - At high dosages, a person’s eyeballs may even begin to spontaneously wiggle back and forth in a rapid motion, causing the vision to become blurry and temporarily out of focus– a condition known as nystagmus.
• Dehydration - Feelings of dry mouth and dehydration are a universal experience with methylone; this effect is a product of an increased heart rate and an extreme motivation to engage in strenuous physical activities. While it is important to avoid becoming dehydrated, especially when out dancing in a hot environment, there have been a number of users suffering from water intoxication through over-drinking so it is advised that users simply sip at water and never over-drink.
• Difficulty urinating - Higher doses of methylone result in an overall difficulty when it comes to urination. This is an effect that is completely temporary and harmless, due to methylone’s promotion of the release of anti-diuretic hormone (ADH). ADH is responsible for regulating urination. This effect can be lessened by simply relaxing, but can be significantly relieved by placing a hot flannel over the genitals to warm them up and encourage blood flow.
• Loss of temperature regulation
• Tactile enhancement

Cognitive effects:

The cognitive effects of methylone can be broken down into six components all of which progressively intensify proportional to dosage. 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.

The most prominent of these cognitive effects generally include:

• Euphoria - Strong emotional euphoria and feelings of happiness are present within methylone and are likely a direct result of serotonin and dopamine release. In comparison to MDMA, it is closer in effects to that of the euphoria felt within amphetamine and mephedrone.
• Empathy, love and sociability enhancement - Although distinct and powerful in its effects, this particular feeling is less pronounced and therapeutic when compared to that of MDMA. It can be described as less forceful and more internal in its manifestation, resulting in feelings of love and empathy that are not necessarily felt as essential to express to others.
• Time distortion - Strong feelings of time compression are common within methylone and speed up the experience of time quite noticeably.
• Unity and interconnectedness - Experiences of unity, oneness and interconnectedness between levels 2 - 3 are common within methylone. This component most consistently manifests itself at high dosages within large crowds at raves and musical events in the form of “becoming one with the crowd.”
• Thought acceleration
• Mindfulness

Physical Health Effects, Potential Addiction and Tolerance:

The toxicity and long term health effects of recreational methylone use does not seem to have been studied in any scientific context and the exact toxic dosage is unknown. This is because methylone is a research chemical with very little history of human usage. Anecdotal evidence from people within the psychonaut community who have tried methylone suggests that there are no negative health effects attributed to simply trying this drug at low to moderate doses or using it very sparingly (but nothing can be completely guaranteed).

Tolerance develops rapidly with repeated usage, so periods of extended use require increasing doses of the drug in order to achieve the same effect. Addiction is a serious risk with heavy recreational use of any stimulant where compulsive redosing is common.

Legal Issues:

• Netherlands: In the Netherlands, methylone is covered under the medicine act. Because methylone is not registered officially, as such, it is forbidden to trade in methylone.
• New Zealand: In New Zealand, although methylone is not explicitly scheduled and falls outside the strict definitions of an “amphetamine analogue” in the Misuse of Drugs Act, it is considered to be “substantially similar” to methcathinone and is thus considered by law enforcement authorities to be a Class C illegal drug.
• United Kingdom: In the UK, methylone has been illegal since the 16/04/2010 revision of the misuse of drugs act.
• Sweden: Methylone has been listed as a schedule I narcotic in Sweden as of Oct 1 of 2010.
• Canada: Although not listed as a Schedule 1 substance, Health Canada reports that methylone falls under the scheduling as an analogue of amphetamine. However, Methylone bears the exact chemical difference between amphetamine and cathinone; cathinone is listed as not being an analogue of amphetamine leading to imply that methylone is unscheduled in Canada.
• United States: As of October 21, 2011 the DEA has issued an emergency ban on methylone. It is illegal to possess and distribute.

Conclusion:

In conclusion, although bk-MDMA is similar to MDMA in high doses, its euphoria is directed inwards rather than forcing the user to project their empathy and love onto others. The dosage is much higher than MDMA in comparison, and it’s a more complex experience due to its different receptor efficacies; there is not simply serotonin happiness, but dirty stimulation too. This substance breakdown was written through collaboration between PsychonautWiki contributors Pjosepherum, Josikins and Oscarette. The full article, including references, is available here.