Construct | [3H]Dihydroalprenolol | Pindolol | ||
---|---|---|---|---|
Kd ± S.E. | Bmax ± S.E. | Ki [S.E. interval] | Hill | |
nM | pmol/mg | nM | ||
WT | 0.20 ± 0.02 | 14.0 ± 4.5 | 0.93 [0.892–0.965] | −1.08 |
D130N | 0.22 ± 0.01 | 1.0 ± 0.2 | 0.92 [0.882–0.960] | −1.15 |
D130A | 0.20 ± 0.02 | 5.8 ± 1.0 | 0.83 [0.813–0.851] | −1.01 |
CAM | 0.21 ± 0.01 | 5.4 ± 1.0 | 0.75 [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.