4-Methylamphetamine
Source: Wikipedia, the free encyclopedia.
Stimulant and anorectic drug of the amphetamine class
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Routes of administration | Oral, intranasal, injection, |
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Elimination half-life | 6-12 hours |
Excretion | Urine |
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4-Methylamphetamine (4-MA; PAL-313; Aptrol; p-TAP) is a
chemical classes
.
In vitro, it acts as a
affinity values of 53.4nM, 22.2nM, and 44.1nM at the serotonin, norepinephrine, and dopamine transporters, respectively.[1] 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 (~18 x baseline) relative to dopamine (~5 x baseline). 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.[2]
4-MA was investigated as an
appetite suppressant in 1952 and was even given a trade name, Aptrol, but development was apparently never completed.[3] More recently it has been reported as a novel designer drug
.
In animal studies, 4-MA was shown to have the lowest rate of self-administration out of a range of similar drugs tested (the others being
3-fluoroamphetamine), likely as a result of having the highest potency for releasing serotonin relative to dopamine.[4][5]
More than a dozen deaths were reported throughout Europe in 2012-2013 after consumption of amphetamine ('speed') contaminated with 4-methylamphetamine.[6]
See also
- 1-(4-Methylphenyl)-2-aminobutane
- 2-Methylamphetamine
- 3-Methylamphetamine
- 4-Methyl-N-methylamphetamine
- 4-Methyl-N-methylcathinone
- 4-Methylphenmetrazine
- 3-Methoxy-4-methylamphetamine
- 3,4-Dimethylamphetamine
- 4-Ethylamphetamine
References
antagonists
receptor agonists
- Beloranib§
- Bimagrumab§
- Desiccated thyroid‡
- Metformin
- Metreleptin
- Naltrexone
- Setmelanotide
- Topiramate
- ZGN-1061
- Zonisamide
- Water
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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Amphetamines |
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Phentermines |
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Cathinones |
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Phenylisobutylamines | |
Phenylalkylpyrrolidines | |
Catecholamines (and close relatives) |
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Miscellaneous |
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