Binding affinity and selectivity ratios of abediterol, salmeterol, formoterol, and indacaterol for the human β1-, β2-, and β3-adrenergic receptors
Affinities are expressed as IC50 (inhibitory concentration at which 50% of the total binding was inhibited). Each value represents the mean ± S.E.M. of at least three independent experiments (n = 3–7).
| Compound | Binding Affinity, IC50 | Binding Selectivity | |||
|---|---|---|---|---|---|
| β1 | β2 | β3 | β1/β2 | β3/β2 | |
| nM | |||||
| Abediterol | 36.2 ± 7.3 | 0.6 ± 0.1 | 3001.2 ± 514.6 | 60 | 5002 |
| Salmeterol | 1781.0 ± 102.3 | 2.7 ± 0.7 | 5996.0 ± 1195.1 | 660 | 2221 |
| Formoterol | 710.6 ± 71.1 | 25.7 ± 3.2 | >10,000 | 28 | >389 |
| Indacaterol | 135.6 ± 4.9 | 34.0 ± 3.2 | 3931.3 ± 815.1 | 4 | 116 |