Figure 5.

Correlation of pEC₅₀ for ligand-induced upregulation and pK_i for CAM β₂-adrenoceptor-Renilla luciferase activity for a range of β₂-adrenoceptor antagonists/inverse agonists. Experiments similar to those described in Figure 4 were conducted using varying concentrations of sotolol (A), betaxolol (B), ICI118551 (C), CGP12177A (D) and propranolol (E). Measured EC₅₀ values for upregulation and estimated K_i values from binding studies were then compared. Data represent means±s.e.mean from three experiments.