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An overview on the biochemistry of the cannabinoid system.

María Gómez-Ruiz, Mariluz Hernández, Rosario De Miguel, Jose A Ramos

Molecular Neurobiology August 2007 DOI: 10.1007/s12035-007-0015-0 (opens in new tab)

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Characteristics Review Peer reviewed
Key findings The review outlines the biochemistry of the endocannabinoid system, describing its receptors, endogenous ligands, and inactivation machinery. It argues that the term "cannabinoid" now extends beyond Cannabis sativa compounds to synthetic cannabinoids, endogenous ligands, and selective receptor antagonists, and attributes the growth of cannabinoid pharmacology to characterization of this modulatory signaling system, which acts mainly in the brain and also in the periphery.

Abstract

About 40 years ago, cannabinoids were considered as the substances responsible for the psychoactive properties of marijuana and other derivatives of Cannabis sativa, whereas their medicinal use remained unexplored. However, with the discovery of the endocannabinoid system 20 years later, the compounds able to modify this system are being reconsidered for their therapeutic potential. Thus, the term "cannabinoid" includes now much more compounds than those present in C. sativa derivatives, for instance, numerous synthetic cannabinoids obtained by modifications from plant-derived cannabinoids or from the compounds that behave as endogenous ligands for the different cannabinoid receptor types. The term "cannabinoid" should also refer to some prototypes of selective antagonists for these receptors. The explanation for this exponential growth in cannabinoid pharmacology is the discovery and characterization of the endocannabinoid signaling system (receptors, ligands, and inactivation system) which plays a modulatory role mainly in the brain but also in the periphery. The objective of the present review article was to give an overview of the present state-of-the-art of biochemistry of the endocannabinoid system. Other authors in this volume will review their functions in the brain, their alterations in a variety of neurological and psychiatric pathologies, and the proposed therapeutic benefits in these diseases of new cannabinoid-related compounds that improve the pharmacological properties of classic cannabinoids.

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