TABLE 1

Affinity and potency values for arylacetamides using GloSensor and Tango

ArylacetamidesG Protein EC50G Protein EmaxArrestin EC50Arrestin EmaxBias Factor
nMnM
Salvinorin A5.183 (−8.29 ± 0.10)99.75.75 (−8.24 ± 0.06)97.21
ICI 199,4411.63 (−8.79 ± 0.07)1010.428 (−9.37 ± 0.05)84.84 Arrestin
ICI 204,4484.22 (−8.38 ± 0.09)1113.28 (−8.48 ± 0.06)77.42 Arrestin
U695935.89 (−8.23 ± 0.07)1096.42 (−8.19 ± 0.09)89.31
GR896960.970 (−9.01 ± 0.11)96.40.259 (−9.60 ± 0.06)92.85 Arrestin
U620661.01 (−9.00 ± 0.05)1036.21 (−8.21 ± 0.10)92.76 G protein
(+)U50,488246 (−6.61 ± 0.12)102959 (−6.02 ± 0.08)92.38 G protein
(−)U50,4880.858 (−9.06 ± 0.07)95.50.822 (−9.09 ± 0.09)94.62 Arrestin
DIPPA14.5 (−7.84 ± 0.09)1118.49 (−8.07 ± 0.07)68.51
N-MPPP4.45 (−8.35 ± 0.09)1092.41 (−8.62 ± 0.06)79.71
BRL 525371.85 (−8.73 ± 0.07)1121.35 (−8.87 ± 0.05)88.91