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Mephedrone, compared with MDMA (ecstasy) and amphetamine, rapidly increases both dopamine and 5-HT levels in nucleus accumbens of awake rats.
Br J Pharmacol. 2011 Dec; 164(8):1949-58.BJ

Abstract

BACKGROUND AND PURPOSE

The designer drug 1-(4-methylphenyl)-2-methylaminopropan-1-one (4-methylmethcathinone, mephedrone) is reported to possess psychostimulant, entactogenic and hallucinogenic effects. The purpose of this study was to examine the effects of acute administration of mephedrone on extracellular levels of dopamine (DA) and 5-HT in the nucleus accumbens of awake rats and compare these effects with those induced by 3,4-methylenedioxymethamphetamine (MDMA, ecstasy) and amphetamine.

EXPERIMENTAL APPROACH

Microdialysis sampling was performed while simultaneously recording locomotor activity in rats and the monoamines were determined by HPLC with electrochemical detection.

KEY RESULTS

Mephedrone (3 mg·kg(-1) s.c.) and (+)-amphetamine (1 mg·kg(-1) s.c.) caused rapid increases in extracellular DA levels of 496% and 412%, respectively, whereas MDMA (3 mg·kg(-1) s.c.) showed only a moderate effect (235%). The corresponding 5-HT levels increased to 941% (mephedrone) and 911% (MDMA), but only to 165% following amphetamine. The calculated t(1/2) values for elimination rate of mephedrone, MDMA and amphetamine-induced increases in extracellular DA levels were 25, 303 and 51 min, the corresponding t(1/2) values for 5-HT were 26, 48 and 84 min, respectively. Locomotor activity was increased most by amphetamine, whereas both mephedrone and MDMA showed about three times lower and shorter-lasting effects.

CONCLUSIONS AND IMPLICATIONS

The neurochemical and functional properties of mephedrone resemble those of MDMA, but it also shows an amphetamine-like effect in that it evokes a rapid release and elimination of DA in the brain reward system, a feature that may contribute to its potent reinforcing properties.

Authors+Show Affiliations

Department of Physiology and Pharmacology, Karolinska Institutet Science Park, Fogdevreten 2a, Stockholm, Sweden. jk@pronexus.seNo 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, Non-U.S. Gov't

Language

eng

PubMed ID

21615721

Citation

Kehr, J, et al. "Mephedrone, Compared With MDMA (ecstasy) and Amphetamine, Rapidly Increases Both Dopamine and 5-HT Levels in Nucleus Accumbens of Awake Rats." British Journal of Pharmacology, vol. 164, no. 8, 2011, pp. 1949-58.
Kehr J, Ichinose F, Yoshitake S, et al. Mephedrone, compared with MDMA (ecstasy) and amphetamine, rapidly increases both dopamine and 5-HT levels in nucleus accumbens of awake rats. Br J Pharmacol. 2011;164(8):1949-58.
Kehr, J., Ichinose, F., Yoshitake, S., Goiny, M., Sievertsson, T., Nyberg, F., & Yoshitake, T. (2011). Mephedrone, compared with MDMA (ecstasy) and amphetamine, rapidly increases both dopamine and 5-HT levels in nucleus accumbens of awake rats. British Journal of Pharmacology, 164(8), 1949-58. https://doi.org/10.1111/j.1476-5381.2011.01499.x
Kehr J, et al. Mephedrone, Compared With MDMA (ecstasy) and Amphetamine, Rapidly Increases Both Dopamine and 5-HT Levels in Nucleus Accumbens of Awake Rats. Br J Pharmacol. 2011;164(8):1949-58. PubMed PMID: 21615721.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Mephedrone, compared with MDMA (ecstasy) and amphetamine, rapidly increases both dopamine and 5-HT levels in nucleus accumbens of awake rats. AU - Kehr,J, AU - Ichinose,F, AU - Yoshitake,S, AU - Goiny,M, AU - Sievertsson,T, AU - Nyberg,F, AU - Yoshitake,T, PY - 2011/5/28/entrez PY - 2011/5/28/pubmed PY - 2012/3/17/medline SP - 1949 EP - 58 JF - British journal of pharmacology JO - Br. J. Pharmacol. VL - 164 IS - 8 N2 - BACKGROUND AND PURPOSE: The designer drug 1-(4-methylphenyl)-2-methylaminopropan-1-one (4-methylmethcathinone, mephedrone) is reported to possess psychostimulant, entactogenic and hallucinogenic effects. The purpose of this study was to examine the effects of acute administration of mephedrone on extracellular levels of dopamine (DA) and 5-HT in the nucleus accumbens of awake rats and compare these effects with those induced by 3,4-methylenedioxymethamphetamine (MDMA, ecstasy) and amphetamine. EXPERIMENTAL APPROACH: Microdialysis sampling was performed while simultaneously recording locomotor activity in rats and the monoamines were determined by HPLC with electrochemical detection. KEY RESULTS: Mephedrone (3 mg·kg(-1) s.c.) and (+)-amphetamine (1 mg·kg(-1) s.c.) caused rapid increases in extracellular DA levels of 496% and 412%, respectively, whereas MDMA (3 mg·kg(-1) s.c.) showed only a moderate effect (235%). The corresponding 5-HT levels increased to 941% (mephedrone) and 911% (MDMA), but only to 165% following amphetamine. The calculated t(1/2) values for elimination rate of mephedrone, MDMA and amphetamine-induced increases in extracellular DA levels were 25, 303 and 51 min, the corresponding t(1/2) values for 5-HT were 26, 48 and 84 min, respectively. Locomotor activity was increased most by amphetamine, whereas both mephedrone and MDMA showed about three times lower and shorter-lasting effects. CONCLUSIONS AND IMPLICATIONS: The neurochemical and functional properties of mephedrone resemble those of MDMA, but it also shows an amphetamine-like effect in that it evokes a rapid release and elimination of DA in the brain reward system, a feature that may contribute to its potent reinforcing properties. SN - 1476-5381 UR - https://www.unboundmedicine.com/medline/citation/21615721/Mephedrone_compared_with_MDMA__ecstasy__and_amphetamine_rapidly_increases_both_dopamine_and_5_HT_levels_in_nucleus_accumbens_of_awake_rats_ L2 - https://doi.org/10.1111/j.1476-5381.2011.01499.x DB - PRIME DP - Unbound Medicine ER -