PSB-CB-27 is a potent, selective antagonist of GPR18 with IC50 of 650 nM, shows no inhibition on GPR55 and low affinity for CB1/CB2 receptors.
PSB-CB-27 showed improved selectivity versus CB receptors as compared to PSB-CB5.
PSB-CB-27 shows a complete blockade of THC-induced GPR18 activation and is thus a superior tool for target validation, compared with partial inhibition by PSB-CB5.
PSB-CB-27 exhibits a pIC50 of 6.2 at the hGPR18 in the β-arrestin recruitment assays.
