cb-2 receptor agonist 3

GP 2A is a selective agonist of CB2 receptor.

(±)19(20)-EDP ethanolamide is an ω-3 endocannabinoid epoxide and cannabinoid (CB) receptor agonist (EC50s = 108 and 280 nM for CB1 and CB2, respectively). It is produced through direct epoxygenation of docosahexaenoyl ethanolamide by cytochrome P450 (CYP) epoxygenases. (±)19(20)-EDP ethanolamide (25 μM) reduces the viability of 143B metastatic osteosarcoma cells. It decreases the production of IL-6 and increases the production of IL-10 when used at concentrations ranging from 2.5 to 10 μM in BV-2 microglia stimulated by LPS and decreases LPS-induced cytotoxicity when used at concentrations ranging from 5 to 10 μM. It also decreases nitrite production when used at a concentration of 7.5 μM, an effect that can be partially reversed by the CB2 receptor antagonist AM630 and the PPARγ antagonist GW 9662 . (±)19(20)-EDP ethanolamide induces vasodilation of isolated preconstricted bovine coronary arteries (ED50 = 1.9 μM) and reduces tube formation by human microvascular endothelial cells (HMVECs) in a Matrigel assay.

(±)-WIN 55,212-2 is a potent aminoalkylindole cannabinoid (CB) receptor agonist with a Ki value of 62.3 and 3.3 nM for human recombinant central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors, respectively. In contrast, the enantiomer (-)-WIN 55,212-3 acts a partial inverse agonist at CB1 (pIC50 = 5.5) and as a competitive neutral antagonist of CB2, reversing the inverse agonism evoked by SR 144528 (pEC50 = 5.3). (+)-WIN 55,212 (mesylate) is a mixture of the two enantiomers, (+)-WIN 55,212-2 and (-)-WIN 55,212-3.