The preclinical pharmacology of mephedrone; not justMDMAby another name
British Journal of Pharmacology – March 24, 2014
Source: OpenAlex
Summary
Mephedrone, a banned stimulant since 2010, may be more addictive than MDMA (ecstasy). In studies with rodents, mephedrone increased locomotor activity and altered body temperature, but these effects were shorter-lived compared to MDMA. Notably, mephedrone does not produce neurotoxic effects on monoamines like MDMA does. It enhances dopamine and serotonin release more significantly than MDMA, with self-administration rates for mephedrone surpassing those of MDMA in various experiments. This highlights its potential for higher abuse liability compared to other similar substances.
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.