TABLE 5.
Affinity and potency values for the RB family of salvinorin derivatives using GloSensor and Tango assays
| RB Salvinorins | G Protein EC50 | G Protein Emax | Arrestin EC50 | Arrestin Emax | Bias Factor |
|---|---|---|---|---|---|
| G Protein | |||||
| nM | nM | ||||
| Salvinorin A | 5.183 (−8.29 ± 0.10) | 99.7 | 5.75 (−8.24 ± 0.06) | 97.2 | 1 |
| Salvinorin B | 73.4 (−7.13 ± 0.08) | 95.9 | 428 (−6.37 ± 0.07) | 115 | 4 G protein |
| RB-64 | 5.29 (−8.27 ± 0.06) | 101 | 391 (−6.41 ± 0.05) | 104 | 35 G protein |
| RB-48 | 8.82 (−8.05 ± 0.07) | 101 | 143 (−6.84 ± 0.09) | 63.2 | 25 G protein |
| RB-55_1 | 119 (−6.93 ± 0.07) | 101 | 1492 (−5.83 ± 0.15) | 52.2 | 22 G protein |
| RB-55_2 | 142 (−6.84 ± 0.10) | 105 | 2284 (−5.64 ± 0.09) | 56.8 | 33 G protein |
| RB 55 | 31.3 (−7.50 ± 0.08) | 103 | 229 (−6.64 ± 0.07) | 86.9 | 8 G protein |
| RB 50 | 166 (−6.78 ± 0.10) | 103 | 3812 (−5.42 ± 0.21) | 89.2 | 69 G protein |
| RB 59 | 35.8 (−7.45 ± 0.10) | 95.7 | 4290 (−5.37 ± 0.13) | 76.6 | 95 G protein |
| RB 65 | 145 (−6.83 ± 0.10) | 95.9 | 2767 (−5.56 ± 0.13) | 42.7 | 29 G protein |