TABLE 4.
Relative duration of binding of existing clinically used and novel β-AR ligands as determined from 3H-CGP12177 whole-cell binding in CHO-β1 cells
| Compound | Human β1-AR |
|
|---|---|---|
| Log shift | n | |
| Bisoprolol | 2.70 ± 0.18 | 4 |
| Carvedilol | 0.31 ± 0.06 | 5 |
| CGP20712A | 1.35 ± 0.04 | 28 |
| ICI118551 | 1.64 ± 0.07 | 24 |
| Nebivolol | 0.26 ± 0.07 | 3 |
| LK204-545 | 2.06 ± 0.08 | 6 |
| NDD-713 | 1.75 ± 0.08 | 9 |
| NDD-825 | 1.62 ± 0.11 | 8 |
The log shift given is the measure of the rightward shift of the washout curve compared with the control curve examined in parallel in each experiment as seen in Fig. 4. A greater shift represents shorter duration ligands, and smaller shifts represent longer duration ligands. Values shown are means ± sem of n separate experiments (n).