1. Drug Discov Today. 2010 Jun;15(11-12):474-83. Epub 2010 Mar 19.

Endocannabinoid biosynthesis and inactivation, from simple to complex.

Muccioli GG.

Bioanalysis and Pharmacology of Bioactive Lipids Laboratory, CHAM7230, Louvain
Drug Research Institute, Université catholique de Louvain, Av. E. Mounier 72,
B-1200 Bruxelles, Belgium. giulio.muccioli@uclouvain.be

Cannabinoid receptors, the primary molecular targets of the endocannabinoid
system, are activated by specific bioactive lipids termed 'endocannabinoids'.
These lipid transmitters are synthesized from cell membrane phospholipids through
multiple pathways and are inactivated by enzymatic hydrolysis, and their levels
are the major parameter driving the endocannabinoid system activity. An in-depth 
understanding of their metabolic pathways is essential to unravel the
endocannabinoid system's role in physiological and pathological situations and to
devise new therapeutic strategies based on the endocannabinoid system. Major
advances both in the characterization of anandamide's and
2-arachidonoylglycerol's biosynthesis and inactivation pathways and in the
discovery of pharmacological tools used to interfere with their metabolism have
been made and are discussed in this review.


PMID: 20304091 [PubMed - indexed for MEDLINE]