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2-Arachidonylglycerol
Other Information:
Canadian
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Chemical Name:(5Z,8Z,11Z,14Z)-5,8,11,14-Eicosatetraenoic acid,
2-hydroxy-1-(hydroxymethyl)ethyl ester
Biological Activity:
Endogenous cannabinoid ligand.
Unlike anandamide and N-palmitoylethanolamine, it acts as a full and potent
agonist at both CB1 and CB2 receptors (Ki
values are 472 and 1400 nM respectively). Found in the brain at concentrations
1000-fold higher than that of anandamide.
Mechoulamet al (1995) Identification of an endogenous
2-monoglyceride, present in canine gut, that binds to cannabinoid receptors.
Biochem.Pharmacol. 50 83. Sugiuraet al (1999)
Evidence that the cannabinoid CB1 receptor is a 2-arachidonoylglycerol
receptor. J.Biol.Chem. 274 2794. Sugiuraet al
(2000) Evidence that 2-arachidonoylglycerol but not N-palmitoylethanolamine or
anandamide is the physiological ligand for the cannabinoid CB2 receptor.
J.Biol.Chem. 275 605.
Highly selective CB2 receptor agonist; Ki values are 0.037 and 363 nM for CB2 and CB1 receptors respectively. Increases P-ERK1/2 expression in HL-60 cells in vitro.
