Methylone

Tēma sadaļā 'Euphoric substances and stimulants', bija izveidotā Charles Darwin, 3/5/14.

  1. TS
    Charles Darwin

    Charles Darwin Guest

    Methylone,

    also known asM1,3,4-
    -N-
    ,MDMC, orbk-MDMA, is an
    and
    of the
    ,
    and
    classes. It was first synthesized by chemists Peyton Jacob III and
    in 1996 for potential use as an antidepressant. Methylone is a close
    of
    , differing by the addition of a β-
    .

    Recreational use



    "Explosion"

    At the end of 2004, a new
    Called "Explosion" appeared in the Netherlands. This drug was sold as a liquid via the internet and in
    "
    ", stores selling at the time non-scheduled, usually becoming illegal within a year of becoming well-known,
    such as
    ,
    and other
    substitutes like
    and
    . The product is advertised as a "room odorizer" and is sold in plastic tubes containing 5 mL of liquid. The tubes cost between €10 and €15 ($13–$20) and do not present any information about the composition of Explosion; they contain only a label saying "Room odorizer Vanilla. Do not ingest" and "Keep away from children. Never use more than one bottle". Users have mentioned ingesting the liquid to reach euphoric stimulating effects similar to those of
    . The label circumvents Dutch regulations for illicit drugs and psychoactive substances when intentionally used for intoxication. Analysis of "Explosion" has confirmed that the active ingredient is methylone. Many other formulations marketed as household chemicals, as well as the pure powder, have been sold.

    Effects

    Reported dosages range from 100 to 250 mg orally. Some respondents say that increasing dose with methylone beyond 100–180 mg causes increased physical effects and does not substantially improve the empathic cognitive effects.

    The effects of methylone may include the following:



    Most of these effects are very similar to those of other
    .

    Resemblance to MDMA

    See also:



    Structural similarities between some Амф-like stimulants and their 3,4-methylenedioxy- derivatives.
    Left:
    ,
    and
    .
    Right:
    ,
    , and methylone
    Methylone resembles MDMA in its behavioural profile, as it substitutes for MDMA in rats trained to discriminate MDMA from saline. Methylone does not substitute for Амф or for the hallucinogenic DOM in animals trained to discriminate between these drugs and saline. Further, also in common with MDMA, methylone acts on monoaminergic systems. In vitro, methylone has one third the potency of MDMA at inhibiting platelet serotonin accumulation and about the same in its inhibiting effects on the dopamine and noradrenaline transporters.

    In spite of these behavioural and pharmacological similarities between methylone and MDMA, the observed subjective effects of both drugs are not completely identical.
    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."

    Pharmacology

    Pharmacodynamics

    Methylone acts as a mixed
    /
    of
    ,
    , and
    . In comparison to MDMA, it has approximately 3x lower
    for the
    , while its affinity for the
    and
    is similar. Notably, methylone's affinity for the
    (VMAT2) is about 13x lower than that of MDMA. The results of these differences in pharmacology relative to MDMA are that methylone is less
    in terms of
    , has more balanced
    effects relative to
    , and behaves more like a reuptake inhibitor like
    than a releaser like
    ; however, methylone has relatively robust releasing capabilities, perhaps due to its ability to
    the
    being similar in potency relative to MDMA.

    Pharmacokinetics

    The two major
    in
    for methylone areN-
    to
    (MDC), and
    followed byO-
    of the 3- or 4-
    to
    (HMMC) or
    (3-OH-4-MeO-MC). When 5 mg/kg of methylone was administered to rats, it was found that around 26% was excreted as HMMC within the first 48 hours (less than 3% excreted unchanged).
     
    Charles Darwin, 3/5/14
    #1