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4-Methylmethcathinone (mephedrone): neuropharmacological effects of a designer stimulant of abuse.
J Pharmacol Exp Ther. 2011 Nov; 339(2):530-6.JP

Abstract

The designer stimulant 4-methylmethcathinone (mephedrone) is among the most popular of the derivatives of the naturally occurring psychostimulant cathinone. Mephedrone has been readily available for legal purchase both online and in some stores and has been promoted by aggressive Web-based marketing. Its abuse in many countries, including the United States, is a serious public health concern. Owing largely to its recent emergence, there are no formal pharmacodynamic or pharmacokinetic studies of mephedrone. Accordingly, the purpose of this study was to evaluate effects of this agent in a rat model. Results revealed that, similar to methylenedioxymethamphetamine, methamphetamine, and methcathinone, repeated mephedrone injections (4× 10 or 25 mg/kg s.c. per injection, 2-h intervals, administered in a pattern used frequently to mimic psychostimulant "binge" treatment) cause a rapid decrease in striatal dopamine (DA) and hippocampal serotonin (5-hydroxytryptamine; 5HT) transporter function. Mephedrone also inhibited both synaptosomal DA and 5HT uptake. Like methylenedioxymethamphetamine, but unlike methamphetamine or methcathinone, repeated mephedrone administrations also caused persistent serotonergic, but not dopaminergic, deficits. However, mephedrone caused DA release from a striatal suspension approaching that of methamphetamine and was self-administered by rodents. A method was developed to assess mephedrone concentrations in rat brain and plasma, and mephedrone levels were determined 1 h after a binge treatment. These data demonstrate that mephedrone has a unique pharmacological profile with both abuse liability and neurotoxic potential.

Authors+Show Affiliations

Department of Pharmacology and Toxicology, University of Utah, 30 South 2000 East, Salt Lake City, UT 84112, USA.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, N.I.H., Extramural

Language

eng

PubMed ID

21810934

Citation

Hadlock, Gregory C., et al. "4-Methylmethcathinone (mephedrone): Neuropharmacological Effects of a Designer Stimulant of Abuse." The Journal of Pharmacology and Experimental Therapeutics, vol. 339, no. 2, 2011, pp. 530-6.
Hadlock GC, Webb KM, McFadden LM, et al. 4-Methylmethcathinone (mephedrone): neuropharmacological effects of a designer stimulant of abuse. J Pharmacol Exp Ther. 2011;339(2):530-6.
Hadlock, G. C., Webb, K. M., McFadden, L. M., Chu, P. W., Ellis, J. D., Allen, S. C., Andrenyak, D. M., Vieira-Brock, P. L., German, C. L., Conrad, K. M., Hoonakker, A. J., Gibb, J. W., Wilkins, D. G., Hanson, G. R., & Fleckenstein, A. E. (2011). 4-Methylmethcathinone (mephedrone): neuropharmacological effects of a designer stimulant of abuse. The Journal of Pharmacology and Experimental Therapeutics, 339(2), 530-6. https://doi.org/10.1124/jpet.111.184119
Hadlock GC, et al. 4-Methylmethcathinone (mephedrone): Neuropharmacological Effects of a Designer Stimulant of Abuse. J Pharmacol Exp Ther. 2011;339(2):530-6. PubMed PMID: 21810934.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - 4-Methylmethcathinone (mephedrone): neuropharmacological effects of a designer stimulant of abuse. AU - Hadlock,Gregory C, AU - Webb,Katy M, AU - McFadden,Lisa M, AU - Chu,Pei Wen, AU - Ellis,Jonathan D, AU - Allen,Scott C, AU - Andrenyak,David M, AU - Vieira-Brock,Paula L, AU - German,Christopher L, AU - Conrad,Kevin M, AU - Hoonakker,Amanda J, AU - Gibb,James W, AU - Wilkins,Diana G, AU - Hanson,Glen R, AU - Fleckenstein,Annette E, Y1 - 2011/08/02/ PY - 2011/8/4/entrez PY - 2011/8/4/pubmed PY - 2012/1/17/medline SP - 530 EP - 6 JF - The Journal of pharmacology and experimental therapeutics JO - J. Pharmacol. Exp. Ther. VL - 339 IS - 2 N2 - The designer stimulant 4-methylmethcathinone (mephedrone) is among the most popular of the derivatives of the naturally occurring psychostimulant cathinone. Mephedrone has been readily available for legal purchase both online and in some stores and has been promoted by aggressive Web-based marketing. Its abuse in many countries, including the United States, is a serious public health concern. Owing largely to its recent emergence, there are no formal pharmacodynamic or pharmacokinetic studies of mephedrone. Accordingly, the purpose of this study was to evaluate effects of this agent in a rat model. Results revealed that, similar to methylenedioxymethamphetamine, methamphetamine, and methcathinone, repeated mephedrone injections (4× 10 or 25 mg/kg s.c. per injection, 2-h intervals, administered in a pattern used frequently to mimic psychostimulant "binge" treatment) cause a rapid decrease in striatal dopamine (DA) and hippocampal serotonin (5-hydroxytryptamine; 5HT) transporter function. Mephedrone also inhibited both synaptosomal DA and 5HT uptake. Like methylenedioxymethamphetamine, but unlike methamphetamine or methcathinone, repeated mephedrone administrations also caused persistent serotonergic, but not dopaminergic, deficits. However, mephedrone caused DA release from a striatal suspension approaching that of methamphetamine and was self-administered by rodents. A method was developed to assess mephedrone concentrations in rat brain and plasma, and mephedrone levels were determined 1 h after a binge treatment. These data demonstrate that mephedrone has a unique pharmacological profile with both abuse liability and neurotoxic potential. SN - 1521-0103 UR - https://www.unboundmedicine.com/medline/citation/21810934/4_Methylmethcathinone__mephedrone_:_neuropharmacological_effects_of_a_designer_stimulant_of_abuse_ L2 - http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=21810934 DB - PRIME DP - Unbound Medicine ER -