Description
2-Arachidonyl glycerol ether (2-AG ether) selectively binds to cannabinoid (CB) receptor 1 (K
is = 21.2 and >3,000 nM for CB
1 and CB
2, respectively, in a radioligand binding assay). It is a potent and selective agonist of CB
1 and GPR55 with EC
50 values of 10, 37, and >30,000 nM for CB
1, GPR55, and CB
2, respectively. 2-AG ether displays the typical tetrad of CB activities in mice. It is more chemically stable than 2-AG , with an endogenous half-life of hours rather than minutes. However, it is at least 10-fold less potent than 2-AG in eliciting typical CB
1-mediated responses. 2-AG ether elicits modest reductions in intraocular pressure in rabbits when administered at doses exceeding 50 μg per eye. It increases aqueous humor outflow
via the CB
1 receptor in the trabecular meshwork. Administration of 2-AG ether to the nucleus accumbens (0.0625-1 μg) increases dietary intake and enhances fat consumption in rats given access to both high-carbohydrate and high-fat diets.
Biological Activity
Endogenous agonist for the GPR55 and CB 1 receptors (EC 50 values are 10 and 37 nM respectively) that displays selectivity over CB 2 receptors (K i values are 21.2 nM and > 3mM at CB 1 and CB 2 respectively). Causes sedation, hypothermia, intestinal immobility and mild antinociception in vivo . Attenuates sensory neurotransmission in rat mesenteric arteries via GPR55. Also available as part of the Endocannabinoid Tocriset™ .
