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Endocannabinoid chemical biology: a tool for the development of novel therapies.

Abstract

The identification of the major psychoactive constituent of Cannabis and marijuana, Delta(9)-tetrahydrocannabinol, opened the way first to the cloning of the G-protein-coupled cannabinoid CB(1) and CB(2) receptors, and then to the isolation and characterisation of their endogenous agonists, the endocannabinoids. Considerable progress has been made in the characterisation of pathways and enzymes for the biosynthesis and degradation of anandamide and 2-arachidonoylglycerol, the two best-known endocannabinoids, as well as of endocannabinoid-related molecules, such as the N-acylethanolamines, which, as in the case of N-palmitoylethanolamine and N-oleoylethanolamine, may interact with other receptor types. However, it is still not fully understood how other plant cannabinoids, of which cannabidiol is the most studied representative, exert their pharmacological effects. Together with these issues, this first review article on the endocannabinoids describes the synthetic pharmacological tools that have been designed so far to interact with the proteins of the 'endocannabinoid system' and that can potentially be used as templates for the development of new therapies.

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  • Publisher Full Text
  • Authors

    Petrosino S, Ligresti A, Di Marzo V

    Source

    Current opinion in chemical biology 13:3 2009 Jun pg 309-20

    MeSH

    Amidohydrolases
    Animals
    Cannabinoid Receptor Agonists
    Cannabinoid Receptor Antagonists
    Cannabinoid Receptor Modulators
    Chemistry, Pharmaceutical
    Drug Discovery
    Endocannabinoids
    Humans
    Lipoprotein Lipase
    Monoacylglycerol Lipases

    Pub Type(s)

    Journal Article
    Review

    Language

    eng

    PubMed ID

    19457702