British Journal of Pharmacology
March 24, 2014
Andrew R. Green, Madeleine V. King, S.e. Shortall et al.
70 citations
Mephedrone, a substituted β-keto amphetamine banned in the UK in 2010, continues to be used recreationally. Users compare its effects to MDMA (ecstasy), but preclinical data reveal key differences. Both drugs enhance locomotor activity and change rectal temperature in rodents, but mephedrone's effects are shorter due to its rapid metabolism and short plasma half-life. Unlike MDMA, mephedrone has no pharmacologically active metabolites and little evidence of inducing neurotoxic decreases in monoamine concentrations. Both drugs induce dopamine and serotonin release, but mephedrone's effect on serotonin release is more marked. Mephedrone shows high abuse liability, supporting self-administration at higher rates than MDMA, and its pharmacological profile differs from other cathinones as well.
British Journal of Pharmacology
October 8, 2012
S.e. Shortall, Andrew R. Green, Km Swift et al.
51 citations
Mephedrone, a synthetic cathinone, produces different effects on body temperature and brain chemistry than MDMA (ecstasy) in rats. MDMA caused sustained decreases in rectal and tail temperature, while mephedrone caused only a transient drop in rectal temperature and a prolonged decrease in tail temperature. In contrast, cathinone and methcathinone raised rectal temperature. MDMA reduced serotonin and certain metabolites in several brain regions, whereas cathinone and methcathinone increased the dopamine metabolite homovanillic acid and serotonin metabolite 5-HIAA in the striatum. Mephedrone increased plasma noradrenaline, which was blocked by certain receptor antagonists. The adverse effects of cathinones in humans cannot be extrapolated from MDMA data.
British Journal of Pharmacology
June 2, 2008
Andrew R. Green
30 citations
Serotonin (5-hydroxytryptamine or 5-HT) was identified as a vasoconstrictor substance by Maurice Rapport in 1949. Gaddum and colleagues soon detected 5-HT in brain and discovered that lysergic acid diethylamide (LSD) antagonized its action in peripheral tissues, leading Gaddum to propose that 5-HT might regulate mood. This review covers the first 20 years of UK scientists' contributions, including developing assays for brain 5-HT, identifying its synthesis and metabolism enzymes, and studying drug effects on brain 5-HT. It describes human LSD experiments, including Gaddum's self-administration, and investigations into 5-HT's role in psychiatric disorders and antidepressant drug effects on 5-HT levels in rodent and human brain.