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Research ArticleArticle

In Vitro Metabolism and Pharmacokinetic Studies on Methylone

Anders Just Pedersen, Trine Hedebrink Petersen and Kristian Linnet
Drug Metabolism and Disposition June 2013, 41 (6) 1247-1255; DOI: https://doi.org/10.1124/dmd.112.050880
Anders Just Pedersen
Section of Forensic Chemistry, Department of Forensic Medicine, Faculty of Health Sciences (A.J.P., K.L.), and Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Copenhagen, Denmark (T.H.P.)
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Trine Hedebrink Petersen
Section of Forensic Chemistry, Department of Forensic Medicine, Faculty of Health Sciences (A.J.P., K.L.), and Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Copenhagen, Denmark (T.H.P.)
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Kristian Linnet
Section of Forensic Chemistry, Department of Forensic Medicine, Faculty of Health Sciences (A.J.P., K.L.), and Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Copenhagen, Denmark (T.H.P.)
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Abstract

Abuse of the stimulant designer drug methylone (methylenedioxymethcathinone) has been documented in most parts of the world. As with many of the new designer drugs that continuously appear in the illicit drug market, little is known about the pharmacokinetics of methylone. Using in vitro studies, CYP2D6 was determined to be the primary enzyme that metabolizes methylone, with minor contributions from CYP1A2, CYP2B6, and CYP2C19. The major metabolite was identified as dihydroxymethcathinone, and the minor metabolites were N-hydroxy-methylone, nor-methylone, and dihydro-methylone. Measuring the formation of the major metabolite, biphasic Michaelis–Menten kinetic parameters were determined: Vmax,1 = 0.046 ± 0.005 (S.E.) nmol/min/mg protein, Km,1 = 19.0 ± 4.2 μM, Vmax,2 = 0.22 ± 0.04 nmol/min/mg protein, and Km,2 = 1953 ± 761 μM; the low-capacity and high-affinity contribution was assigned to the activity of CYP2D6. Additionally, a time-dependent loss of CYP2D6 activity was observed when the enzyme was preincubated with methylone, reaching a maximum rate of inactivation at high methylone concentrations, indicating that methylone is a mechanism-based inhibitor of CYP2D6. The inactivation parameters were determined to be KI = 15.1 ± 3.4 (S.E.) μM and kinact = 0.075 ± 0.005 minute−1.

Footnotes

    • Received January 2, 2013.
    • Accepted April 1, 2013.
  • dx.doi.org/10.1124/dmd.112.050880.

  • Copyright © 2013 by The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 41 (6)
Drug Metabolism and Disposition
Vol. 41, Issue 6
1 Jun 2013
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Research ArticleArticle

In Vitro Metabolism and Kinetics Studies on Methylone

Anders Just Pedersen, Trine Hedebrink Petersen and Kristian Linnet
Drug Metabolism and Disposition June 1, 2013, 41 (6) 1247-1255; DOI: https://doi.org/10.1124/dmd.112.050880

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Research ArticleArticle

In Vitro Metabolism and Kinetics Studies on Methylone

Anders Just Pedersen, Trine Hedebrink Petersen and Kristian Linnet
Drug Metabolism and Disposition June 1, 2013, 41 (6) 1247-1255; DOI: https://doi.org/10.1124/dmd.112.050880
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