TABLE 1

Potencies and efficacies of ligands for mouse κ-opioid receptor in vitro

DrugG Protein ActivationArrestin MobilizationBias Factor
nM
Salvinorin AEC50 = 4.73 (−8.33 ± 0.04)EC50 = 10.5 (−7.98 ± 0.05)1
Emax = 101Emax = 93.6
U69593EC50 = 3.68 (−8.43 ± 0.04)EC50 = 25.4 (−7.59 ± 0.03)3 G protein
Emax = 99.7Emax = 100
RB-64EC50 = 5.22 (−7.92 ± 0.05)EC50 = 1130 (−5.94 ± 0.03)96 G protein
Emax = 99.0Emax = 126