TABLE 2

Functional β2 selectivity of agonists against the different human β-adrenergic receptor subtypes

CHO cells selectively expressing the human adrenergic β1-, β2-, and β3-receptors were stimulated with increasing concentrations of agonists (0.03–10,000 nM), and cAMP levels were quantified as described under Materials and Methods. Data are reported as mean ± S.E.M. of three independent experiments. EC50 is the concentration required to do 50% of the maximal effect (versus the reference agonists epinephrine, formoterol hemifurate, and ZD7114 for the β1, β2, and β3 assays, respectively).

CompoundcAMP Production, EC50Functional Cellular Selectivity
β1β2β3β12β32
nM
Abediterol6.0 ± 0.70.15 ± 0.034.1 ± 0.64028
Salmeterol84.0 ± 10.50.16 ± 0.0327.4 ± 2.2525171
Formoterol2.5 ± 0.50.19 ± 0.010.6 ± 0.0133
Indacaterol1.8 ± 0.30.96 ± 0.211.7 ± 0.122