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Journal of Pharmacology and Experimental Therapeutics

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OtherBEHAVIORAL PHARMACOLOGY

Increased Locomotor Activity Induced by Heroin in Mice: Pharmacokinetic Demonstration of Heroin Acting as a Prodrug for the Mediator 6-Monoacetylmorphine in Vivo

Jannike Mørch Andersen, Åse Ripel, Fernando Boix, Per Trygve Normann and Jørg Mørland
Journal of Pharmacology and Experimental Therapeutics October 2009, 331 (1) 153-161; DOI: https://doi.org/10.1124/jpet.109.152462
Jannike Mørch Andersen
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Åse Ripel
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Fernando Boix
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Per Trygve Normann
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Jørg Mørland
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Abstract

We investigated the relative importance of heroin and its metabolites in eliciting a behavioral response in mice by studying the relationship between concentrations of heroin, 6-monoacetylmorphine (6MAM), and morphine in brain tissue and the effects on locomotor activity. Low doses (subcutaneous) of heroin (≤5 μmol/kg) or 6MAM (≤15 μmol/kg) made the mice run significantly more than mice given equimolar doses of morphine. There were no differences in the response between heroin and 6MAM, although we observed a shift to the left of the dose-response curve for the maximal response of heroin. The behavioral responses were abolished by pretreatment with 1 mg/kg naltrexone. Heroin was detected in brain tissue after injection, but the levels were low and its presence too short-lived to be responsible for the behavioral response observed. The concentration of 6MAM in brain tissue increased shortly after administration of both heroin and 6MAM and the concentration changes during the first hour roughly reflected the changes in locomotor activity. Both the maximal and the total concentration of 6MAM were higher after administration of heroin than after administration of 6MAM itself. The morphine concentration increased slowly after injection and could not explain the immediate behavioral response. In summary, the locomotor activity response after injection of heroin was mediated by 6MAM, which increased shortly after administration. Heroin acted as an effective prodrug. The concentration of morphine was too low to stimulate the immediate response observed but might have an effect on the later part of the heroin-induced behavioral response curve.

  • 6MAM, 6-monoacetylmorphine
  • M6G, morphine-6-glucuronide
  • M3G, morphine-3-glucuronide
  • LC-MS/MS, liquid chromatography-tandem mass spectrometry
  • AUC, area under the curve
  • BBB, blood-brain barrier

Footnotes

  • This study was supported in part by the Norwegian Research Council [Grant 170534/v40].

  • Article, publication date, and citation information can be found at http://jpet.aspetjournals.org.

  • ABBREVIATIONS:.

    • Received March 3, 2009.
    • Accepted June 17, 2009.
  • © 2009 by The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 381 (3)
Journal of Pharmacology and Experimental Therapeutics
Vol. 381, Issue 3
1 Jun 2022
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OtherBEHAVIORAL PHARMACOLOGY

Increased Locomotor Activity Induced by Heroin in Mice: Pharmacokinetic Demonstration of Heroin Acting as a Prodrug for the Mediator 6-Monoacetylmorphine in Vivo

Jannike Mørch Andersen, Åse Ripel, Fernando Boix, Per Trygve Normann and Jørg Mørland
Journal of Pharmacology and Experimental Therapeutics October 1, 2009, 331 (1) 153-161; DOI: https://doi.org/10.1124/jpet.109.152462

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OtherBEHAVIORAL PHARMACOLOGY

Increased Locomotor Activity Induced by Heroin in Mice: Pharmacokinetic Demonstration of Heroin Acting as a Prodrug for the Mediator 6-Monoacetylmorphine in Vivo

Jannike Mørch Andersen, Åse Ripel, Fernando Boix, Per Trygve Normann and Jørg Mørland
Journal of Pharmacology and Experimental Therapeutics October 1, 2009, 331 (1) 153-161; DOI: https://doi.org/10.1124/jpet.109.152462
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