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Noladin ether
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Canadian
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Chemical Name:2-[(5Z,8Z,11Z,14Z)-Eicosatetraenyloxy]-1,3-propanediol
Biological Activity:
Endogenous
agonist for the CB1 receptor (Ki = 21.2 nM). Has low
affinity for CB2 receptors (Ki > 3 μM). Causes sedation, hypothermia,
intestinal immobility and mild antinociception in vivo. Attenuates sensory
neurotransmission in rat mesenteric arteries via a non-CB1/CB2
Gi/o-linked receptor.
Sugiura
et al (1999) Evidence that the cannabinoid
CB1 receptor is a 2-arachidonoylglycerol receptor. J.Biol.Chem. 274
2794. Suhara et al (2000) Synthesis and biological activities of
2-arachidonoylglycerol, an endogenous cannabinoid receptor ligand, and its
metabolically stable ether-linked analogues. Chem.Pharm.Bull.48903.
Hanuset al (2001) 2-Arachidonyl glyceryl ether, an endogenous agonist
of the cannabinoid CB1 receptor. Proc.Natl.Acad.Sci.USA 98
3662. Duncanet al (2004) Noladin ether, a putative
endocannabinoid, attenuates sensory neurotransmission in the rat isolated
mesenteric arterial bed via a non-CB1/CB2 Gi/o
linked receptor. Br.J.Pharmacol. 142 509.
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.
