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Mechanism of action of two new synthetic drugs unravelled for the first time

Date:
April 22, 2015
Source:
Medical University of Vienna
Summary:
Substances such as 4-MEC and 4-MEPP belong to the category of new hybrid cathinone derivatives and have a highly stimulant and euphoria-inducing effect, similar to the synthetic drug mephedrone, which was banned in Austria five years ago. Until now, the mechanisms by which these two drugs worked have been unknown. Scientists have now been able, through an international cooperation agreement, to unravel this mechanism for the first time.
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Substances such as 4-MEC and 4-MEPP belong to the category of new hybrid cathinone derivatives and have a highly stimulant and euphoria-inducing effect, similar to the synthetic drug mephedrone, which was banned in Austria five years ago. Until now, the mechanisms by which these two drugs worked have been unknown. Scientists at the MedUni Vienna have now been able, through an international cooperation agreement, to unravel this mechanism for the first time.

The two drugs 4-MEC and 4-MEPP, which are primarily taken via the nasal and oral route, belong to the group of amphetamines in the second generation of chemically modified cathinone derivatives. The basic cathinone structure occurs naturally in the "khat" plant, which is mostly grown on plantations and consumed in the Horn of Africa, Somalia and the Yemen. Cathinone has central stimulating, euphoria-inducing and psychotropic properties. Khat itself, taken on its own, has only a slightly intoxicating effect, similar to that of a glass or two of beer.

Researchers led by primary author Kusumika Saha from the Institute of Pharmacology at the MedUni Vienna have now been able to demonstrate that 4-MEC (4-Methyl-N-Ethylcathinone) works in two ways, depending on which neurotransmitter transporter it binds to in the brain. "If the substance docks to the serotonin transporter, it acts like amphetamine. If it docks to the dopamine transporter, however, it acts like cocaine," explains Harald Sitte from the Institute of Pharmacology at the MedUni Vienna. It is therefore currently difficult to assess what effect it will have on the consumer, or which effect characteristic will prevail.

In the case of 4-MEPP (4-Methyl-α-pyrrolidinopropiophenone), it was discovered that it acts like a blocker similar to cocaine on dopamine as well as serotonin transporters, comparable with the "zombie drug" MDPV (3.4-Methylenedioxypyrovalerone), which can cause tremendous loss of control and aggression if taken.

International paper with a high-calibre audience

The cover of the journal Neuropsychopharmacology was dedicated to the paper, and the work carried out in close collaboration with the National Institute of Drug Abuse (NIDA) in Baltimore (USA), was also featured by the "Faculty of 1000," giving it a high-calibre international audience too. The "Faculty of 1000" is a review database listing more than 3,500 specialist magazines from the field of medicine and biology.


Story Source:

Materials provided by Medical University of Vienna. Note: Content may be edited for style and length.


Journal Reference:

  1. Kusumika Saha, John S Partilla, Kurt R Lehner, Amir Seddik, Thomas Stockner, Marion Holy, Walter Sandtner, Gerhard F Ecker, Harald H Sitte, Michael H Baumann. ‘Second-Generation’ Mephedrone Analogs, 4-MEC and 4-MePPP, Differentially Affect Monoamine Transporter Function. Neuropsychopharmacology, 2014; 40 (6): 1321 DOI: 10.1038/npp.2014.325

Cite This Page:

Medical University of Vienna. "Mechanism of action of two new synthetic drugs unravelled for the first time." ScienceDaily. ScienceDaily, 22 April 2015. <www.sciencedaily.com/releases/2015/04/150422084226.htm>.
Medical University of Vienna. (2015, April 22). Mechanism of action of two new synthetic drugs unravelled for the first time. ScienceDaily. Retrieved May 23, 2017 from www.sciencedaily.com/releases/2015/04/150422084226.htm
Medical University of Vienna. "Mechanism of action of two new synthetic drugs unravelled for the first time." ScienceDaily. www.sciencedaily.com/releases/2015/04/150422084226.htm (accessed May 23, 2017).

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