4-Methylamphetamine


4-Methylamphetamine, also known by the former proposed brand name Aptrol, is a stimulant and anorectic drug of the amphetamine family. It is structurally related to mephedrone.

Pharmacology

In vitro, 4-methylamphetamine acts as a potent and well-balanced serotonin, norepinephrine, and dopamine releasing agent with values of 53.4nM, 22.2nM, and 44.1nM at the serotonin, norepinephrine, and dopamine transporters, respectively. Receptor interaction data for 4-methylamphetamine have also been reported.
However, more recent in vivo studies that involved performing microdialysis on rats showed a different trend. These studies showed that 4-methylamphetamine is much more potent at elevating serotonin relative to dopamine. The authors speculated that this is because 5-HT release dampens DA release through some mechanism. For example, it was suggested that a possible cause for this could be activation of 5HT2C receptors since this is known to inhibit DA release. In addition there are alternative explanations such as 5-HT release then going on to encourage GABA release, which has an inhibitory effect on DA neurons.
In animal studies, 4-MA was shown to have the lowest rate of self-administration out of a range of similar drugs tested, likely as a result of having the highest potency for releasing serotonin relative to dopamine.

Society and culture

More than a dozen deaths were reported throughout Europe in 2012-2013 after consumption of amphetamine contaminated with 4-methylamphetamine.

Research

4-MA was investigated as an appetite suppressant in 1952 and was even given a trade name, Aptrol, but development was apparently never completed. More recently it has been reported as a novel designer drug.