CB1R Allosteric modulator 4 is an effective and positive modulator of cannabinoid type-1 (CB1R), exhibiting significant biological activity. This compound inhibits the production of cAMP and demonstrates strong β-arrestin-2 recruitment [1].

CB1R is the most abundant G-protein coupled receptors (GPCR) in the CNS, CB1R involves in regulating physiological processes, from neurotransmission to energy metabolism [1]. CB1R Allosteric modulator 4 (compound 66b) (0.10 nM-10μM; 30 min) exerts inhibition of forskolin-stimulated cellular cAMP production in CHO hCB1R with an EC 50 value of 0.05 μM [1]. CB1R Allosteric modulator 4 (0.10 nM-10μM; 90 min) acts function for β-arrestin-2 recruitment in hCB1R-CHO-K1 cells with an EC 50 value of 0.163 μM [1]. CB1R Allosteric modulator 4 (1.6-200 μM; 2 h) improves aqueous solubility with good biological activity, and shows kinetic water solubility with solubility limit of 3.13 μM [1].