cb2 receptor agonist 3

GP 2A is a selective agonist of CB2 receptor.

CB2 receptor agonist 2 (ZINC72105556) is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor, Ki = 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2.

SCH-336 is a CB2 receptor agonist (Ki-1.8 nM, EC50-2 nM) with effective, selective, and oral activity. SCH-336 is also bioactive against CB1 receptor, and is 100 times more selective to CB2 receptor than CB1. SCH-336 reduced the binding of guanosine 5' -3-o -(sulfur) triphosphate to the membrane containing hCB, inhibited BaF3 CB2 cell migration, inhibited leukocyte migration in mouse delayed hypersensitivity models, and inhibited antigen-induced pulmonary eosinophilia in mouse allergy models.

CB2 receptor agonist 8 (Compound 17) is an agonist of the cannabinoid receptor 2 (CB2 receptor). It shows cytotoxicity in U87, RPMI 8226, HL-60, and L929 cells with IC50 values of 91.03, 16.29, 23.51, and 564.6 μM, respectively. CB2 receptor agonist 8 activates caspase 3 7, increases the expression of pro-apoptotic genes BAX, BAD, BIM, and the tumor suppressor gene p53, and induces apoptosis in U87 cells. Additionally, it inhibits the migration of U87 cells.

Arachidonylcyclopropylamide (AM1241) is a highly effective and selective agonist for the CB2R. This compound specifically targets the CB2 receptor, making it a valuable tool for research and therapeutic applications that exploit CB2-specific pathways without affecting CB1 receptors.

(±)10(11)-EDP ethanolamide is an ω-3 endocannabinoid epoxide and cannabinoid (CB) receptor agonist (EC50s = 0.43 and 22.5 nM for CB1 and CB2 receptors, respectively). It is produced though direct epoxygenation of docosahexaenoyl ethanolamide by cytochrome P450 (CYP) epoxygenases. 10,11-EDP epoxide (12.5 and 25 μM) reduces the viability of 143B metastatic osteosarcoma cells. It induces apoptosis and inhibits cell migration in a wound-healing assay in 143B, MG63, and HOS osteosarcoma cells. (±)10(11)-EDP ethanolamide also reduces tube formation by human umbilical vein endothelial cells (HUVECs) in a Matrigel assay.

(±)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.

GW405833 hydrochloride, a potent and selective agonist of the cannabinoid-2 (CB2) receptor (EC 50 = 0.65 nM; maximum inhibition = 44.6%), exhibits significant antihyperalgesic effects in various rodent pain models [1] [2] [3].

RVD-Hpα acetate is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. Increases intracellular Ca2+ levels in cells expressing CB1 receptors in vitro. Also high affinity CB2 positive allosteric modulator (Ki