cb2 receptor agonist 3

GP 2A is a selective agonist of CB2 receptor.

CB2 receptor agonist 2 (ZINC72105556) 是有效和选择性的 CB2 受体激动剂。对 CB2 的 Ki 为 8.5 nM。CB2 receptor agonist 2 对 CB2 具有高亲和力和选择性。

CB2receptor agonist 8 (Compound 17) 是一种大麻素受体 2 (CB2 receptor) 激动剂。它在 U87、RPMI 8226、HL-60 和 L929 细胞系中表现出细胞毒性，IC50分别为 91.03、16.29、23.51 和 564.6 μM。该化合物激活 caspase3 7，增加促凋亡基因 BAX、BAD、BIM 和肿瘤抑制基因 p53 的表达，并在 U87 细胞中诱导细胞凋亡 (apoptosis)，同时抑制 U87 细胞的迁移。

CB2R激动剂, 其化学式为C25H28N6O3S，分子量为508.6 g mol。作为一种高效且具有选择性的CB2R激动剂，该化合物表现出在医疗研究中应用的潜力。其结构包含吡咯并[2,3-b]吡啶-3-胺环，与CB2受体的结合力强。在体外试验中，这种化合物的EC50值为22 nM，体现了其高度选择性。

SCH-336是一种 CB2受体激动剂(Ki-1.8 nM, EC50-2 nM)，具有有效性，选择性和口服活性。SCH-336对 CB1受体也具有生物活性，对CB2受体的选择性是CB1的100倍。SCH-336能够减少鸟苷5'-3- o -(硫)三磷酸与含hCB 的膜的结合，抑制 BaF3 CB2 细胞迁移，抑制小鼠延迟型超敏反应模型中的白细胞迁移，抑制小鼠过敏模型中抗原诱导的肺嗜酸性粒细胞增多。

(±)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.

(±)-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.

GW405833 hydrochloride是高效选择性的大麻素-2 (CB2)受体激动剂，具有EC50值为0.65 nM和最大抑制率为44.6%。在多种啮齿动物疼痛模型中，该化合物展现了显著的镇痛效果。

RVD-Hpα acetate(1193362-76-3 free base) 是人血加压素的 N 末端延伸形式，可作为选择性 CB1 受体激动剂。增加体外表达 CB1 受体的细胞中的细胞内 Ca2+ 水平。也是高亲和力 CB2 正变构调节剂 (Ki = 50 nM)。