CB2R antagonist 3 is a selective antagonist of cannabinoid type 2 receptor (CB2R). CB2R antagonist 3 has high affinity for human CB2R and specific selectivity for CB1R. CB2R antagonist 3 can be combined with CB65 , the activator of CB2R. CB2R antagonist 3 effectively up-regulates the expression of anti-inflammatory cytokines and down-regulates the expression of pro-inflammatory cytokines.
CB2R antagonist 3 (compound 10a) (1 and 10 µM; 24 h) significantly reduces the TNF-α, IFN-γ, IL-1β, IL-6 pro-inflammatory cytokines expression and increases the IL-10 anti-inflammatory cytokines expression in monocytes and macrophages when combined with activator CB65 under the presence of lipopolysaccharide[1].
References:
[1]. Graziano G, et al. N-adamantyl-anthranil amide derivatives: New selective ligands for the cannabinoid receptor subtype 2 (CB2R). Eur J Med Chem. 2023 Feb 15;248:115109.