cb1 antagonist 2

CB1 antagonist 2 (AM4113) 是一种 caimabinoid 1 拮抗剂，在体内抑制 CB1 的IC50值为 25.5 nM。

CB1 antagonist 4 是外周选择性大麻素受体1型受体拮抗剂。它减少精神病副作用的倾向。它对大脑的渗透率有限，以降低或防止 CNS 不良反应，并保留潜在的抗肥胖作用。

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。

Ibipinabant (SLV319) 是一种有效，选择性和具有口服活性的大麻素 CB1 受体 (cannabinoid CB1 receptor) 的拮抗剂，Ki 值为 7.8 nM。Ibipinabant 对 CB1 的选择性超过 CB2 (Ki=7943 nM) 的 1000 倍以上。Ibipinabant 可用于肥胖和糖尿病的研究。

O-2050 是一种高亲和力的大麻素CB1受体拮抗剂，Ki 为 2.5 nM。O-2050 抑制大麻素 CB2受体，Ki 为 0.2 nM。O-2050 减少了小鼠的食物摄入量，并且引起小鼠运动。

(±)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.

AZD-2207 is a cannabinoid receptor CB1 antagonist and highly lipophilic compound for the treatment of type 2 diabetes mellitus and obesity.

AZD-1175 is a cannabinoid receptor CB1 antagonist and highly lipophilic compound for the treatment of type 2 diabetes and obesity.

Isopropyl dodec-11-enylfluorophosphonate (IDEFP) 为有机磷酯类化合物，能抑制中枢大麻素受体 (cannabinoid receptor) (CB1) 并具有相似的效力抑制FAAH（IC50s = 2 nM）。