NOLADIN ETHER Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
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.
Verwenden
HU 310 is an endogenous GPR55 and CB1 receptors agonist. HU 310 has been shown to induce hyperglycia in rats. HU 310 can be used to investigate the biological roles of GPR55 and CB1 receptors.
Definition
ChEBI: A monoalkylglycerol that is the 2-O-arachidonyl derivative of glycerol.
Biologische Aktivität
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™ .
NOLADIN ETHER Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
