The preclinical pharmacology of mephedrone; not justMDMAby another name
Andrew R. Green, Madeleine V. King, Sinead E Shortall, K.c.f. Fone
British Journal of Pharmacology March 24, 2014 DOI: 10.1111/bph.12628 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Review Peer reviewed |
|---|---|
| Topics | MDMA |
| Keywords | Mephedrone Pharmacology Methamphetamine Monoamine neurotransmitter Dopamine Drug |
| Citations | 70 |
| Key findings | Mephedrone differs from MDMA in its pharmacological profile, behavioral effects, and neurotoxic effects, and also differs from other cathinones. |
Abstract
The substituted β‐keto amphetamine mephedrone (4‐methylmethcathinone) was banned in the UK in A pril 2010 but continues to be used recreationally in the UK and elsewhere. Users have compared its psychoactive effects to those of 3,4‐methylenedioxymethamphetamine ( MDMA , ‘ecstasy’). This review critically examines the preclinical data on mephedrone that have appeared over the last 2–3 years and, where relevant, compares the pharmacological effects of mephedrone in experimental animals with those obtained following MDMA administration. Both mephedrone and MDMA enhance locomotor activity and change rectal temperature in rodents. However, both of these responses are of short duration following mephedrone compared with MDMA probably because mephedrone has a short plasma half‐life and rapid metabolism. Mephedrone appears to have no pharmacologically active metabolites, unlike MDMA . There is also little evidence that mephedrone induces a neurotoxic decrease in monoamine concentration in rat or mouse brain, again in contrast to MDMA . Mephedrone and MDMA both induce release of dopamine and 5‐ HT in the brain as shown by in vivo and in vitro studies. The effect on 5‐ HT release in vivo is more marked with mephedrone even though both drugs have similar affinity for the dopamine and 5‐HT transporters in vitro . The profile of action of mephedrone on monoamine receptors and transporters suggests it could have a high abuse liability and several studies have found that mephedrone supports self‐administration at a higher rate than MDMA . Overall, current data suggest that mephedrone not only differs from MDMA in its pharmacological profile, behavioural and neurotoxic effects, but also differs from other cathinones.
Comparable studies
Other narrative reviews on MDMA, most cited first.
| Study | Year | Design | Participants |
|---|---|---|---|
| Human Pharmacology of MDMA | 2004 | Review | |
| Human psychopharmacology of Ecstasy (MDMA): a review of 15 years of empirical research | 2001 | Review | |
| 3,4‐Methylenedioxymethamphetamine (MDMA, “Ecstasy”): pharmacology and toxicology in animals and humans | 1994 | Review | |
| (±)3,4-Methylenedioxymethamphetamine (‘Ecstasy’)-Induced Serotonin Neurotoxicity: Studies in Animals | 2000 | Review | |
| Amphetamine toxicities | 2010 | Review |
Citations in the library
Cited by 17
- Novel psychoactive substances (designer drugs): overview and pharmacology of modulators of monoamine signalling Swiss Medical Weekly January 11, 2015
- Effect fingerprinting of new psychoactive substances (NPS): What can we learn from in vitro data? Pharmacology & Therapeutics February 1, 2018
- Novel Psychoactive Substances—Recent Progress on Neuropharmacological Mechanisms of Action for Selected Drugs Frontiers in Psychiatry August 18, 2017
- Mephedrone (4-Methylmethcathinone): Acute Behavioral Effects, Hyperthermic, and Pharmacokinetic Profile in Rats Frontiers in Psychiatry January 10, 2018
- Mephedrone and Alcohol Interactions in Humans Frontiers in Pharmacology January 28, 2020
and 12 more in the library
Cites 46
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- 'Eve' and 'Ecstasy'. A report of five deaths associated with the use of MDEA and MDMA JAMA March 27, 1987
- The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain. European Journal of Pharmacology March 22, 2007
- 3,4-Methylenedioxymethamphetamine (MDMA) neurotoxicity in rats: a reappraisal of past and present findings Psychopharmacology March 15, 2006
- Instability of the ecstasy market and a new kid on the block: mephedrone Journal of Psychopharmacology September 8, 2010
and 41 more in the library