IUPHAR/BPS Guide to Pharmacology CITE
https://doi.org/10.2218/gtopdb/F943/2021.3
Endocannabinoid turnover in GtoPdb v.2021.3
Stephen P.H. Alexander1,
Patrick Doherty2,
Christopher J. Fowler3,
Jürg Gertsch4 and
Mario van der Stelt5
- University of Nottingham, UK
- King's College London, UK
- University Hospital of Umeå, Sweden
- University of Bern, Switzerland
- Leiden University, The Netherlands
Abstract
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 [28]. FABP5 (Q01469) has been suggested to act as a canonical intracellular endocannabinoid transporter in vivo [17]. 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, [70]). A transacylation enzyme which forms N-acylphosphatidylethanolamines has been identified as a cytosolic enzyme, PLA2G4E (Q3MJ16) [62]. In vitro experiments indicate that the endocannabinoids are also substrates for oxidative metabolism via cyclooxygenase, lipoxygenase and cytochrome P450 enzyme activities [5, 23, 72].
Contents
This is a citation summary for Endocannabinoid turnover in the
Guide to Pharmacology
database (GtoPdb). It exists purely as an adjunct to the database to
facilitate the recognition of citations to and from the database by
citation analyzers. Readers will almost certainly want to visit the
relevant sections of the database which are given here under database
links.
GtoPdb is an expert-driven
guide to pharmacological targets and the substances that act on them.
GtoPdb is a reference work which is most usefully represented as an
on-line database. As in any publication this work should be
appropriately cited, and the papers it cites should also be
recognized. This document provides a citation for the relevant parts
of the database, and also provides a reference list for the research
cited by those parts. For further details see [12].
Please note that the database version for the citations given in
GtoPdb are to the most recent preceding version
in which the family or its subfamilies and targets were substantially
changed. The links below are to the current version. If you
need to consult the cited version, rather than the most recent version, please contact
the GtoPdb curators.
Database links
Endocannabinoid turnover
https://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=943
N-Acylethanolamine turnover
https://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=273
Enzymes
NAPE-PLD(N-Acylphosphatidylethanolamine-phospholipase D)
https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1398
FAAH(Fatty acid amide hydrolase)
https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1400
FAAH2(Fatty acid amide hydrolase-2)
https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1401
NAAA(N-Acylethanolamine acid amidase)
https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1402
2-Acylglycerol ester turnover
https://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=944
Enzymes
DAGLα(Diacylglycerol lipase α)
https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1396
DAGLβ(Diacylglycerol lipase β)
https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1397
MAGL(Monoacylglycerol lipase)
https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1399
ABHD2(αβ-Hydrolase 2)
https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=3147
ABHD6(αβ-Hydrolase 6)
https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2919
ABHD12(αβ-Hydrolase 12)
https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=3070
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