CCG-63802 is a reversible, allosteric inhibitor of regulator of G-protein signaling (RGS) proteins with a potency order of RGS4 > 19 = 16 > 8 >> 7.
CCG-63802 inhibits the Gαo-RGS4 interaction with IC50 of 1.9 uM, does not inhibit Gα binding to RGS7, 2- to 10-fold more potent at RGS4 than on the other closely related R4 family members, RGS8 and RGS16.
CCG-63802 decreases neuropathic hyperalgesia and restores cannabinoid CB1 receptor signalling in PSNL rats.
