TABLE 5

Affinity and potency values for the RB family of salvinorin derivatives using GloSensor and Tango assays

RB SalvinorinsG Protein EC50G Protein EmaxArrestin EC50Arrestin EmaxBias Factor
G Protein
nMnM
Salvinorin A5.183 (−8.29 ± 0.10)99.75.75 (−8.24 ± 0.06)97.21
Salvinorin B73.4 (−7.13 ± 0.08)95.9428 (−6.37 ± 0.07)1154 G protein
RB-645.29 (−8.27 ± 0.06)101391 (−6.41 ± 0.05)10435 G protein
RB-488.82 (−8.05 ± 0.07)101143 (−6.84 ± 0.09)63.225 G protein
RB-55_1119 (−6.93 ± 0.07)1011492 (−5.83 ± 0.15)52.222 G protein
RB-55_2142 (−6.84 ± 0.10)1052284 (−5.64 ± 0.09)56.833 G protein
RB 5531.3 (−7.50 ± 0.08)103229 (−6.64 ± 0.07)86.98 G protein
RB 50166 (−6.78 ± 0.10)1033812 (−5.42 ± 0.21)89.269 G protein
RB 5935.8 (−7.45 ± 0.10)95.74290 (−5.37 ± 0.13)76.695 G protein
RB 65145 (−6.83 ± 0.10)95.92767 (−5.56 ± 0.13)42.729 G protein