Table 1.
Functional selectivity profile of Nitro-I, Met-I, OTV1, and OTV2 from BRET assays in the agonist mode
| 5-HT | Nitro-I | Met-I | OTV1 | OTV2 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| pEC50 | Emax | logτ/KA | pEC50 | Emax | logτ/KA | pEC50 | Emax | logτ/KA | pEC50 | Emax | logτ/KA | pEC50 | Emax | logτ/KA | |
| Gαq | 9.75 ± 0.23 | 101.10 ± 2.37 | 9.70 ± 0.15 | 9.65 ± 0.19 | 102.50 ± 9.81 | 9.67 ± 0.20 | 9.55 ± 0.31 | 98.16 ± 12.19 | 9.57 ± 0.39 | 5.38 ± 0.08 | 86.62 ± 3.72 | 5.28 ± 0.11 | 8.35 ± 0.19 | 75.20 ± 5.12 | 8.24 ± 0.14 |
| Gα11 | 10.26 ± 0.08 | 98.03 ± 3.46 | 9.46 ± 0.06 | 9.96 ± 0.23 | 78.67 ± 6.99 | 9.13 ± 0.13 | 8.88 ± 0.11 | 79.73 ± 3.08 | 8.60 ± 0.12 | 5.41 ± 0.10 | 127.30 ± 11.26 | 5.93 ± 0.15 | 9.56 ± 0.12 | 80.31 ± 3.35 | 8.92 ± 0.12 |
| Gα14 | 9.30 ± 0.10 | 98.44 ± 5.21 | 9.14 ± 0.09 | 8.72 ± 0.15 | 102.90 ± 5.67 | 8.73 ± 0.14 | 8.72 ± 0.11 | 98.77 ± 4.13 | 8.72 ± 0.13 | 5.72 ± 0.13 | 94.48 ± 5.94 | 5.64 ± 0.15 | 9.18 ± 0.25 | 90.79 ± 6.32 | 9.13 ± 0.14 |
| Gα15 | 8.10 ± 0.08 | 99.36 ± 3.22 | 8.03 ± 0.09 | 7.61 ± 0.13 | 107.80 ± 4.62 | 7.66 ± 1.03 | 7.22 ± 0.27 | 98.48 ± 5.40 | 7.21 ± 0.10 | NA | NA | NA | 7.55 ± 0.33 | 60.05 ± 6.63 | 7.68 ± 0.04 |
| Gαi1 | 8.12 ± 0.17 | 99.92 ± 6.02 | 8.16 ± 0.15 | 6.78 ± 0.09 | 73.92 ± 2.88 | 6.42 ± 0.15 | 7.73 ± 0.15 | 87.12 ± 4.55 | 7.56 ± 0.15 | 6.71 ± 0.28 | 23.21 ± 2.96 | 5.59 ± 0.44 | 7.96 ± 0.25 | 76.81 ± 6.93 | 7.65 ± 0.18 |
| Gαi2 | 6.71 ± 0.08 | 99.95 ± 3.55 | 6.70 ± 0.15 | 7.69 ± 0.22 | 54.55 ± 4.28 | 6.73 ± 0.61 | 7.75 ± 0.16 | 50.40 ± 2.84 | 6.90 ± 0.60 | NA | 8.50 ± 0.38 | 25.05 ± 3.43 | 7.23 ± 0.70 | ||
| Gαi3 | 7.16 ± 0.10 | 100 ± 3.89 | 7.20 ± 0.10 | 7.91 ± 0.15 | 54.48 ± 3.07 | 7.07 ± 0.18 | 7.47 ± 0.13 | 56.76 ± 2.50 | 6.88 ± 0.17 | NA | 8.45 ± 0.31 | 42.55 ± 4.58 | 7.70 ± 0.23 | ||
| GαoA | 7.02 ± 0.08 | 99.99 ± 3.33 | 7.01 ± 0.15 | 7.27 ± 0.24 | 51.01 ± 4.45 | 6.64 ± 0.51 | 7.14 ± 0.19 | 47.38 ± 3.50 | 6.25 ± 0.33 | NA | 8.35 ± 0.25 | 29.67 ± 2.68 | 7.76 ± 0.51 | ||
| GαoB | 6.98 ± 0.08 | 99.85 ± 3.46 | 7.05 ± 0.11 | 7.25 ± 0.23 | 45.76 ± 3.87 | 6.57 ± 0.24 | 7.12 ± 0.16 | 47.46 ± 2.89 | 6.63 ± 0.23 | NA | 8.04 ± 0.45 | 40.55 ± 6.64 | 7.18 ± 0.27 | ||
| Gαz | 8.00 ± 0.08 | 94.48 ± 3.32 | 8.13 ± 0.08 | 7.36 ± 0.14 | 100.30 ± 5.06 | 8.69 ± 0.13 | 7.20 ± 0.13 | 82.95 ± 4.19 | 8.55 ± 0.10 | 8.12 ± 1.81 | 16.44 ± 1.52 | 4.67 ± 0.90 | 8.12 ± 0.21 | 61.83 ± 5.17 | 7.89 ± 0.31 |
| β-arrestin1 | 6.71 ± 0.06 | 99.31 ± 2.59 | 6.88 ± 0.05 | 6.65 ± 0.09 | 46.59 ± 1.95 | 6.32 ± 0.14 | 6.44 ± 0.08 | 38.18 ± 1.40 | 6.04 ± 0.17 | NA | 4.80 ± 0.17 | 76.65 ± 9.22 | 4.37 ± 0.10 | ||
| β-arrestin2 | 6.75 ± 0.04 | 99.70 ± 1.85 | 6.84 ± 0.05 | 6.55 ± 0.11 | 43.78 ± 2.15 | 6.15 ± 0.12 | 6.02 ± 0.05 | 44.96 ± 1.10 | 5.63 ± 0.12 | NA | 6.32 ± 0.15 | 45.50 ± 3.22 | 5.44 ± 0.13 | ||
NA no activity. Data represent mean ± SEM of 3 independent experiments.