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Endocannabinoid turnover in GtoPdb v.2026.1

Title: Endocannabinoid turnover in GtoPdb v.2026.1
Authors: Alexander, Stephen P.H.; Doherty, Patrick; Fowler, Christopher J.; Gertsch, Jürg; van der Stelt, Mario
Source: IUPHAR/BPS Guide to Pharmacology CITE; Vol. 2026 No. 1 (2026) ; 2633-1020
Publisher Information: University of Edinburgh
Publication Year: 2026
Description: 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 [32]. FABP5 (Q01469) has been suggested to act as a canonical intracellular endocannabinoid transporter in vivo [19]. 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, [80]). A transacylation enzyme which forms N-acylphosphatidylethanolamines has been identified as a cytosolic enzyme, PLA2G4E (Q3MJ16) [71]. In vitro experiments indicate that the endocannabinoids are also substrates for oxidative metabolism via cyclooxygenase, lipoxygenase and cytochrome P450 enzyme activities [6, 26, 82].
Document Type: article in journal/newspaper
File Description: application/pdf; text/html
Language: English
Relation: https://journals.ed.ac.uk/gtopdb-cite/article/view/12148/15046; https://journals.ed.ac.uk/gtopdb-cite/article/view/12148/15044; https://journals.ed.ac.uk/gtopdb-cite/article/view/12148/15045
DOI: 10.2218/gtopdb/F943/2026.1
Availability: https://journals.ed.ac.uk/gtopdb-cite/article/view/12148; https://doi.org/10.2218/gtopdb/F943/2026.1
Rights: Copyright (c) 2026 The authors ; http://creativecommons.org/licenses/by-sa/4.0
Accession Number: edsbas.F1B68F53
Database: BASE