CB1R Allosteric modulator 4

CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment[1].

Research Areas >> Others

Signaling Pathways >> GPCR/G Protein >> Cannabinoid Receptor

hCB1-R

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 EC50 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 EC50 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].

[1]. Schaffer PC, et al. Focused structure-activity relationship profiling around the 2-phenylindole scaffold of a cannabinoid type-1 receptor agonist-positive allosteric modulator: site-III aromatic-ring congeners with enhanced activity and solubility. Bioorg Med Chem. 2020 Nov 1;28(21):115727.