The Endocannabinoid System: Its General Strategy Of Action, Tools

Jacob Bell

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The endocannabinoid system: Its general strategy of action, tools for its pharmacological manipulation and potential therapeutic exploitation

Vincenzo Di Marzo Corresponding Author Contact Information, E-mail The Corresponding Author
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Endocannabinoid Research Group, Institute of Biomolecular Chemistry, Consiglio Nazionale delle Ricerche, Via Campi Flegrei 34, Comprensorio Olivetti, 80078 Pozzuoli, Naples, Italy

Received 28 January 2009; Accepted 19 February 2009. Available online 4 March 2009.
Abstract

The endocannabinoid signalling system includes: (1) at least two G-protein-coupled receptors, known as the cannabinoid CB1 and CB2 receptors and discovered following studies on the mechanism of action of Δ9-tetrahydrocannabinol, the major psychoactive principle of the hemp plant Cannabis sativa; (2) the endogenous agonists at these receptors, known as endocannabinoids, of which anandamide and 2-arachidonoylglycerol are the best known; and (3) proteins and enzymes for the regulation of endocannabinoid levels and action at receptors. The endocannabinoid system is quite widespread in mammalian tissues and cells and appears to play a pro-homeostatic role by being activated following transient or chronic perturbation of homeostasis, and by regulating in a local way the levels and action of other chemical signals. Compounds that selectively manipulate the action and levels of endocannabinoids at their targets have been and are being developed, and represent templates for potential new therapeutic drugs.

Keywords: Cannabinoid; Endocannabinoid; Vanilloid; Inhibitors; Homeostasis; CB1; CB2; TRPV1; Anandamide; 2-Arachidonoylglycerol; FAAH; MAGL; DAGL


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