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Research ArticleABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION

Carrier-Mediated Uptake of the Endogenous Cannabinoid Anandamide in RBL-2H3 Cells

Fariborz Rakhshan, Theresa A. Day, Randy D. Blakely and Eric L. Barker
Journal of Pharmacology and Experimental Therapeutics March 2000, 292 (3) 960-967;
Fariborz Rakhshan
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Theresa A. Day
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Randy D. Blakely
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Eric L. Barker
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Abstract

Anandamide (N-arachidonylethanolamide) is an endogenous cannabinoid that mimics the pharmacologic effects of Δ9-tetrahydrocannabinol, the major bioactive substance in marijuana. Anandamide appears to be synthesized, released, and inactivated by mechanisms similar to those for other neurotransmitters. Of interest to the present studies are reports that anandamide undergoes carrier-mediated uptake into neuronal or glial cells after release, followed by rapid intracellular degradation by the intracellular fatty acid amidohydrolase. In addition to effects in the brain, anandamide has multiple effects in the periphery, particularly on cells of the immune system that express both a peripheral cannabinoid receptor and amidohydrolase enzyme. We have performed a detailed characterization of anandamide uptake in the cognate mast cell line RBL-2H3 to test the hypothesis that the uptake system in peripheral cells is also carrier-mediated and functionally similar to that observed in the central nervous system. RBL-2H3 cells exhibited robust, saturable transport of [3H]anandamide that was both time- and temperature-sensitive. This transport activity was not dependent on extracellular ion gradients for uptake and was inhibited selectively by other fatty acid-derived molecules, anandamide congeners, and the psychoactive cannabinoids such as Δ9-tetrahydrocannabinol. We conclude that anandamide transport in the RBL-2H3 cells is carrier-mediated, and uptake in peripheral cells is functionally and pharmacologically identical with that observed in neurons and astrocytes.

Footnotes

  • Send reprint requests to: Eric L. Barker, Ph.D., Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University School of Pharmacy, 1333 R. Heine Pharmacy Bldg., West Lafayette, IN 47907. E-mail: ericb{at}pharmacy.purdue.edu

  • ↵1 This work was supported in part by a research grant from Bristol-Myers Squibb.

  • Abbreviations:
    2-AG
    2-arachidonylglycerol
    THC
    tetrahydrocannabinol
    11-OH-Δ9-THC
    11-hydroxy-nor-Δ9-THC
    FAAH
    fatty acid amidohydrolase
    AM404
    N-(4-hydroxyphenyl)-arachidonamide
    KRH
    Krebs-Ringer-HEPES
    PMSF
    phenylmethylsulfonyl fluoride
    ATFK
    arachidonyl trifluoromethyl ketone
    MAFP
    methyl arachidonyl fluorophosphonate
    • Received September 2, 1999.
    • Accepted December 4, 1999.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 292 (3)
Journal of Pharmacology and Experimental Therapeutics
Vol. 292, Issue 3
1 Mar 2000
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Research ArticleABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION

Carrier-Mediated Uptake of the Endogenous Cannabinoid Anandamide in RBL-2H3 Cells

Fariborz Rakhshan, Theresa A. Day, Randy D. Blakely and Eric L. Barker
Journal of Pharmacology and Experimental Therapeutics March 1, 2000, 292 (3) 960-967;

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Research ArticleABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION

Carrier-Mediated Uptake of the Endogenous Cannabinoid Anandamide in RBL-2H3 Cells

Fariborz Rakhshan, Theresa A. Day, Randy D. Blakely and Eric L. Barker
Journal of Pharmacology and Experimental Therapeutics March 1, 2000, 292 (3) 960-967;
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