Table 2.
Functional properties of emerging β2-adrenoceptor agonists against the three human β-adrenoceptor subtypes
| Agonist | β1 | β2 | β3 | Selectivity for β2 over β1 | ||||
|---|---|---|---|---|---|---|---|---|
| pEC50 | IA | pEC50 | IA | pEC50 | IA | Reference | ||
| Indacaterol | 6.60 ± 0.24 | 16 ± 2 | 8.06 ± 0.02 | 73 ± 1 | 6.72 ± 0.13 | 113 ± 7 | 1.46 | Battram et al., 2006 |
| Olodaterol | 7.55 ± 0.08 | 52 ± 8 | 9.93 ± 0.07 | 88 ± 2 | 6.57 ± 0.08 | 81 ± 2 | 2.38 | Bouyssou et al., 2010a |
| Vilanterol | 6.4 ± 0.1 | 9.4 ± 0.0 | 6.1 ± 0.2 | 3.0 | Procopiou et al., 2010 | |||
| Carmoterol | 10.19 ± 0.15 | 88.6 ± 4.1 | Rosethorne et al., 2010 | |||||
pEC50 is the negative logarithm of the molar drug concentration that produces a cAMP response equal to 50% of its maximal response. IA is the percentage of isoprenaline-induced maximal response. Selectivity for β2 over β1 expressed as pEC50 at β2-adrenoceptor – pEC50 at β1-adrenoceptor.