Ki values of β-subtype-selective antagonists from competition binding experiments with [125I]CYP
| Ligand | High-Affinity β-AR Sites | Low-Affinity β-AR Sites | ||
|---|---|---|---|---|
| Ki3-a | Hill Slopeb | Ki | Hill Slope | |
| nM | nM | |||
| CGP 20712A | 114.1 ± 16.5 | −0.88 ± 0.20 | 1783.0 ± 293.0 | −0.73 ± 0.17 |
| ICI 118551 | 30.4 ± 9.7 | −0.55 ± 0.18 | 680.0 ± 220.0 | −0.56 ± 0.10 |
| SR 59230A | 853.3 ± 120 | −0.63 ± 0.15 | 48.1 ± 14.3 | −0.86 ± 0.14 |
↵3-a Ki values were determined by the Cheng-Prusoff equation as described under Materials and Methods.
b Hill slope was determined using GraphPad Prism 3.0. The 95% confidence intervals of the Hill slope included the value of −1.0 for each ligand.