CB2R/FAAH modulator-1, a cannabinoid type 2 receptor (CB2R) agonist, is also a fatty acid amide hydrolase (FAAH) inhibitor (IC50=4 μM) that reduces the production of pro-inflammatory and anti-inflammatory cytokines and is commonly used in inflammation studies. The Kis for CB2R and CB1R are 14.8 nM and 241.3 nM, respectively.

CB1 receptor:241.3 nM (Kis), CB1 receptor:489 nM (EC50), FAAH:4 μM, CB2 receptor:123.6 nM (EC50), CB2 receptor:14.8 nM (Kis)

CB2R/FAAH modulator-1 在未刺激的单核细胞和巨噬细胞中降低了促炎细胞因子TNFα、IFN-γ、IL-1β和IL6的产生[1]。