Endocannabinoid Turnover

Adv Pharmacol. 2017:80:31-66. doi: 10.1016/bs.apha.2017.03.006. Epub 2017 May 25.

Abstract

In this review, we consider the biosynthetic, hydrolytic, and oxidative metabolism of the endocannabinoids anandamide and 2-arachidonoylglycerol. We describe the enzymes associated with these events and their characterization. We identify the inhibitor profile for these enzymes and the status of therapeutic exploitation, which to date has been limited to clinical trials for fatty acid amide hydrolase inhibitors. To bring the review to a close, we consider whether point block of a single enzyme is likely to be the most successful approach for therapeutic exploitation of the endocannabinoid system.

Keywords: 2-Arachidonoylglycerol; Anandamide; Diacylglycerol lipase; Fatty acid amide hydrolase; Monoacylglycerol lipase; N-acylphosphatidylethanolamine phospholipase D.

Publication types

  • Review

MeSH terms

  • Animals
  • Endocannabinoids / biosynthesis
  • Endocannabinoids / metabolism*
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Lipoprotein Lipase / antagonists & inhibitors
  • Lipoprotein Lipase / metabolism
  • Oxidation-Reduction
  • Signal Transduction / drug effects
  • Synapses / drug effects
  • Synapses / metabolism

Substances

  • Endocannabinoids
  • Enzyme Inhibitors
  • Lipoprotein Lipase