TABLE 3

Functional activity of 5-HOB and formoterol in primary cells with endogenous expression of β-ARs

Emax values were determined relative to formoterol, where formoterol was defined as 100%. The values are expressed as mean ± S.E.M. of at least four independent experiments, each performed with seven concentrations of compounds (10-fold dilutions) in triplicates.

cAMP Response5-HOBFormoterol
EC50EmaxEC50Emax
nM%nM%
Skeletal muscle myotubesRat1.9 ± 0.4104 ± 0.80.1 ± 0.02100 ± 0.0
Dog2.1 ± 0.289 ± 0.80.6 ± 0.03100 ± 0.0
Monkey5.1 ± 0.890 ± 3.71.5 ± 0.37100 ± 0.0
Human1.7 ± 0.196 ± 0.30.3 ± 0.01100 ± 0.0
CardiomyocytesRat4.4 ± 0.572 ± 0.31.6 ± 0.13100 ± 0.0
Human iPS-derived3.4 ± 0.284 ± 2.50.5 ± 0.03100 ± 0.0