cb2 receptor agonist 2

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。

CB2 receptor agonist 9 (Compound 33) 是一种有效的口服大麻素受体 2 (CB2 receptor) 激动剂，EC50 为 16.2 nM。CB2 receptor agonist 9 能抑制 TNF-α、IL-1β 和 IL-6 的表达，并在 DDS 诱导的小鼠急性结肠炎模型中显示抗炎活性。

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。

GP 2A is a selective agonist of CB2 receptor.

GP 1a 是cannabinoid receptor 2（CB2）的强效激动剂（EC50=7.1),是在cAMP、GTPγS 和β-arrestin 招募试验中显示的。GP 1a 对CB2受体的选择性约为CB1受体的30倍，且在体外增加HL-60细胞的P-ERK1 2表达。GP 1a 对皮肤伤口愈合有益。GP 1a 可抑制炎症和纤维生成，同时促进上皮的重新形成。

WIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) 是 cannabinoid receptor 激动剂，对人重组 CB1 受体(Ki:62.3 nM) 和 CB2 受体 (Ki:3.3 nM)。

Cannabigerol 是一种植物大麻素，是一种高亲和力 α2-肾上腺素能受体激动剂、中度亲和力 5-HT1A 受体拮抗剂和低亲和力 CB1 CB2受体拮抗剂。它可降低眼压，有潜力治疗青光眼。

GW842166X 是一种选择性 cannabinoid receptor 2 激活剂，IC50=63 nM。

Olorinab (APD 371) (APD 371) 是大麻素受体 2 型 (CB2) 强有效的、选择性的全激动剂，其对 hCB2 的EC50 值为 6.2 nM。

Tedalinab is an effective and selective cannabinoid receptor 2 agonist. Tedalinab has the potential for neuropathic pain and osteoarthritis treatment. Tedalinab has >4700-fold functional selectivity for CB2 over CB1.

MDA7 是一种选择性激动剂，主要作用于大麻素受体 2 (cannabinoid receptor 2)。在激活方面，其在人体CB2受体和大鼠CB2受体中的EC50分别为128 nM和67.4 nM。此化合物对CB2受体展现出良好的亲和力，对人体和大鼠受体的Ki分别为422 nM和238 nM。此外，MDA7在大鼠模型中表现出镇痛活性。

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。

LEI-101 是有效的、选择性的、具有口服活性的大麻素CB2受体激动剂。LEI-101对 hCB2 的 pEC50值为 8，对 hERG 的 pKi 值小于 4。LEI-101 与 CB2 受体的结合能力比 CB1 强100 倍。LEI-101 具有炎症及氧化应激相关疾病的治疗潜力。

(±)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.

Noladin ether (2-AG ether) 是一种具有选择性和高效性的大麻素 CB1 受体激动剂，通过非 CB1 CB2 G（i o） 连接受体减弱大鼠离体肠系膜动脉床中的感觉神经传递，以浓度依赖性方式减弱感觉神经源性松弛。

Arachidonoyl 2-chloroethylamide (ACEA) is a potent and selective cannabinoid (CB) receptor 1 agonist with Ki values of 1.4 and >2,000 nM for CB1 and CB2 receptors, respectively. In whole animal experiments, ACEA induces hypothermia in mice with the same efficacy as arachidonoyl ethanolamide , in spite of its higher affinity for the CB1 receptor. These data have been interpreted to indicate that ACEA may be a substrate for fatty acid amide hydrolase (FAAH), and thus only transiently available in whole animal experiments.

(±)-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.

Vicasinabin, a potent agonist of cannabinoid receptor 2 (CB2), exhibits promising potential for researching chronic pain, atherosclerosis, regulation of bone mass, neuroinflammation, and related human diseases.

S-777469 是一种选择性的、口服具有活力的大麻素 2 型受体(CB2)激动剂 (Ki: 36 nM)。S-777469 能够剂量依赖性地明显抑制化合物 48 80 诱导的小鼠抓挠行为。S-777469 兴奋 CB2，抑制瘙痒信号的传递，显示出止痒效果。

BML-190 (Indomethacin morpholinylamide) 是一种 CB2 受体的配体，其对 CB2 受体 (Ki:435 nM) 和 CB1受体 (Ki> 2 μM)。

GW833972 is a CB2 Agonist. GW 833972A inhibited capsaicin-induced depolarization of the human and guinea-pig and prostaglandin E(2) (PGE(2)) and hypertonic saline-induced depolarization of the guinea-pig isolated vagus nerve in vitro. GW 833972A also inhibited citric acid-induced cough but not plasma extravasation in the guinea-pig and this effect was blocked by a CB(2) receptor antagonist.

LY2828360 是一种作用缓慢的、有效的 G 蛋白偏倚的大麻素受体 2(CB2)激动剂，能够抑制 cAMP 的积累并激活 ERK1 2 通路。

RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selectiveCB1receptoragonist. RVD-Hpα TFA increases intracellular Ca2+levels in cells expressingCB1receptors in vitro. RVD-Hpα TFA also high affinityCB2positive allosteric modulator (Ki=50 nM).

MCHB-1, a potent agonist of the human cannabinoid 2 (CB2) receptor (EC50= 0.52 nM), demonstrates high selectivity for CB2 over CB1 (Kis = 3.7 and 110 nM, respectively), distinguishing itself from similar benzimidazole compounds that significantly alleviate peripheral pain while minimizing central nervous system side effects in mice.