Endocannabinoid turnover (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database

  • Stephen P.H. Alexander University of Nottingham https://orcid.org/0000-0003-4417-497X
  • Patrick Doherty King's College London
  • Christopher J. Fowler University Hospital of Umeå
  • Jürg Gertsch University of Bern
  • Mario van der Stelt Leiden University


The principle endocannabinoids are 2-acylglycerol esters, such as 2-arachidonoylglycerol (2-AG), and N-acylethanolamines, such as anandamide (N-arachidonoylethanolamine, AEA). The glycerol esters and ethanolamides are synthesised and hydrolysed by parallel, independent pathways. Mechanisms for release and re-uptake of endocannabinoids are unclear, although potent and selective inhibitors of facilitated diffusion of endocannabinoids across cell membranes have been developed [19]. FABP5 (Q01469) has been suggested to act as a canonical intracellular endocannabinoid transporter in vivo [12]. For the generation of 2-arachidonoylglycerol, the key enzyme involved is diacylglycerol lipase (DAGL), whilst several routes for anandamide synthesis have been described, the best characterized of which involves N-acylphosphatidylethanolamine-phospholipase D (NAPE-PLD, [49]). A transacylation enzyme which forms N-acylphosphatidylethanolamines has recently been identified as a cytosolic enzyme, PLA2G4E (Q3MJ16) [43]. In vitro experiments indicate that the endocannabinoids are also substrates for oxidative metabolism via cyclooxygenase, lipoxygenase and cytochrome P450 enzyme activities [4, 16, 51].
How to Cite
Alexander, S. P., Doherty, P., Fowler, C. J., Gertsch, J. and van der Stelt, M. (2019) “Endocannabinoid turnover (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database”, IUPHAR/BPS Guide to Pharmacology CITE, 2019(4). doi: 10.2218/gtopdb/F943/2019.4.