cb1 antagonist 2

CB1 antagonist 2 (AM4113) is caimabinoid 1 (CB1) antagonist which inhibits CB1 in vivo with an IC50 of 25.5 nM.

CB1 antagonist 4 is an antagonist of cannabinoid receptor type 1 (CB1), with potential for the treatment of obesity and type 2 diabetes.

Cannabigerol is a high affinity α±2-adrenergic receptor agonist, moderate affinity 5-HT1A receptor antagonist, and low affinity CB1 receptor antagonist ; also binds to the CB2 receptor; it can relieve interocular pressure, which may be of benefit in the treatment of glaucoma.

Ibipinabant (SLV319) is a potent, selective, and orally active cannabinoid CB1 receptor antagonist, with a K_i of 7.8 nM and over 1000-fold selectivity for CB1 compared to CB2 (K_i = 7943 nM). It is utilized in obesity and diabetes research [1] [2] [3].

O-2050 is a high-affinity cannabinoid CB1 receptor antagonist with a Ki of 2.5 nM and inhibits the cannabinoid CB2 receptor with a Ki of 0.2 nM. O-2050 decreased food intake and stimulated locomotion in mice [1].

(±)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.

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) is an organophosphorus ester that serves as a central cannabinoid receptor (CB1) antagonist and equally inhibits fatty acid amide hydrolase (FAAH), both with an IC50 value of 2 nM [1].