Table 2.
Effect of a maximally effective concentration of indacaterol on the potency and intrinsic activity values of a panel of glucocorticoid receptor ligands to promote GRE-dependent transcription in BEAS-2B reporter cells
| Glucocorticoid | n | p[A]50 −Indacaterol | Fold induction −Indacaterol | αa | p[A]50 +Indacaterol | Fold Induction +Indacaterolb | αa |
|---|---|---|---|---|---|---|---|
| Fluticasone furoate | 4 | 8.73 ± 0.05 | 16.4 ± 0.80 | 1 | 8.66 ± 0.08 | 44.1 ± 3.30 | 1.00 |
| Dexamethasone | 4 | 7.79 ± 0.07 | 14.9 ± 0.46 | 0.96 | 7.80 ± 0.06 | 41.7 ± 2.54 | 0.94 |
| GSK 9027 | 5 | 6.77 ± 0.17 | 12.8 ± 2.10 | 0.77 | 7.03 ± 0.05 | 30.1 ± 2.73 | 0.68 |
| Des-ciclesonide | 5 | 8.39 ± 0.03 | 9.22 ± 0.24 | 0.53 | 8.32 ± 0.05 | 25.5 ± 1.15 | 0.57 |
| GW 870086X | 8 | 7.72 ± 0.05 | 6.67 ± 0.22 | 0.36 | 7.72 ± 0.04 | 14.3 ± 0.67 | 0.31 |
| Mifepristone | 8 | 7.67 ± 0.42 | 1.26 ± 0.09 | 0.02 | 7.75 ± 0.16 | 1.81 ± 0.06 | 0.02 |
| Org 34517 | 6 | Inactive | 0.99b | 0 | 8.02b | 1.24b | 0.006 |