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Ligands that target cannabinoid receptors in the brain: from THC to anandamide and beyond.

Abstract

A major finding--that (-)-trans-Delta(9)-tetrahydrocannabinol (Delta(9)-THC) is largely responsible for the psychotropic effects of cannabis--prompted research in the 1970s and 1980s that led to the discovery that this plant cannabinoid acts through at least two types of cannabinoid receptor, CB(1) and CB(2), and that Delta(9)-THC and other compounds that target either or both of these receptors as agonists or antagonists have important therapeutic applications. It also led to the discovery that mammalian tissues can themselves synthesize and release agonists for cannabinoid receptors, the first of these to be discovered being arachidonoylethanolamide (anandamide) and 2-arachidonoylglycerol. These 'endocannabinoids' are released onto their receptors in a manner that appears to maintain homeostasis within the central nervous system and sometimes either to oppose or to mediate or exacerbate the unwanted effects of certain disorders. This review provides an overview of the pharmacology of cannabinoid receptors and their ligands. It also describes actual and potential clinical uses both for cannabinoid receptor agonists and antagonists and for compounds that affect the activation of cannabinoid receptors less directly, for example by inhibiting the enzymatic hydrolysis of endocannabinoids following their release.

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  • Publisher Full Text
  • Authors+Show Affiliations

    School of Medical Sciences, Institute of Medical Sciences, University of Aberdeen, Aberdeen, UK. rgp@abdn.ac.uk

    Source

    Addiction biology 13:2 2008 Jun pg 147-59

    MeSH

    Animals
    Arachidonic Acids
    Brain
    Cannabinoid Receptor Modulators
    Cannabinoids
    Dronabinol
    Endocannabinoids
    Glycerides
    Humans
    Marijuana Abuse
    Polyunsaturated Alkamides
    Receptor, Cannabinoid, CB1
    Receptor, Cannabinoid, CB2

    Pub Type(s)

    Journal Article
    Review

    Language

    eng

    PubMed ID

    18482430

    Citation

    Pertwee, Roger G.. "Ligands That Target Cannabinoid Receptors in the Brain: From THC to Anandamide and Beyond." Addiction Biology, vol. 13, no. 2, 2008, pp. 147-59.
    Pertwee RG. Ligands that target cannabinoid receptors in the brain: from THC to anandamide and beyond. Addict Biol. 2008;13(2):147-59.
    Pertwee, R. G. (2008). Ligands that target cannabinoid receptors in the brain: from THC to anandamide and beyond. Addiction Biology, 13(2), pp. 147-59. doi:10.1111/j.1369-1600.2008.00108.x.
    Pertwee RG. Ligands That Target Cannabinoid Receptors in the Brain: From THC to Anandamide and Beyond. Addict Biol. 2008;13(2):147-59. PubMed PMID: 18482430.
    * Article titles in AMA citation format should be in sentence-case
    TY - JOUR T1 - Ligands that target cannabinoid receptors in the brain: from THC to anandamide and beyond. A1 - Pertwee,Roger G, PY - 2008/5/17/pubmed PY - 2008/7/9/medline PY - 2008/5/17/entrez SP - 147 EP - 59 JF - Addiction biology JO - Addict Biol VL - 13 IS - 2 N2 - A major finding--that (-)-trans-Delta(9)-tetrahydrocannabinol (Delta(9)-THC) is largely responsible for the psychotropic effects of cannabis--prompted research in the 1970s and 1980s that led to the discovery that this plant cannabinoid acts through at least two types of cannabinoid receptor, CB(1) and CB(2), and that Delta(9)-THC and other compounds that target either or both of these receptors as agonists or antagonists have important therapeutic applications. It also led to the discovery that mammalian tissues can themselves synthesize and release agonists for cannabinoid receptors, the first of these to be discovered being arachidonoylethanolamide (anandamide) and 2-arachidonoylglycerol. These 'endocannabinoids' are released onto their receptors in a manner that appears to maintain homeostasis within the central nervous system and sometimes either to oppose or to mediate or exacerbate the unwanted effects of certain disorders. This review provides an overview of the pharmacology of cannabinoid receptors and their ligands. It also describes actual and potential clinical uses both for cannabinoid receptor agonists and antagonists and for compounds that affect the activation of cannabinoid receptors less directly, for example by inhibiting the enzymatic hydrolysis of endocannabinoids following their release. SN - 1369-1600 UR - https://www.unboundmedicine.com/medline/citation/18482430/Ligands_that_target_cannabinoid_receptors_in_the_brain:_from_THC_to_anandamide_and_beyond_ L2 - https://doi.org/10.1111/j.1369-1600.2008.00108.x DB - PRIME DP - Unbound Medicine ER -