Table 1

Binding properties of WT and mutant β2ARs

Construct[3H]DihydroalprenololPindolol
Kd ± S.E.Bmax ± S.E.Ki [S.E. interval]Hill
nM pmol/mg nM
WT0.20  ± 0.0214.0  ± 4.50.93 [0.892–0.965]−1.08
D130N0.22  ± 0.011.0  ± 0.20.92 [0.882–0.960]−1.15
D130A0.20  ± 0.025.8  ± 1.00.83 [0.813–0.851]−1.01
CAM0.21  ± 0.015.4  ± 1.00.75 [0.708–0.787]−0.90

Saturation and competition binding assays were performed on membranes derived from COS-7 cells transiently expressing the WT or mutants’ receptors. Values are from three to five independent experiments performed in triplicate. The IC50 values used for calculations of K i values were obtained from means of pIC50 values determined by nonlinear regression analysis and the S.E. interval from pIC50 ± S.E.