Comparison of pharmacological properties of several β-AR antagonists against human β1-, β2-, and β3-AR expressed in CHO cells
| Ki4-a | |||
|---|---|---|---|
| β1-AR | β2-AR | β3-AR | |
| nM | |||
| (±)-Metoprolol | 226 ± 125 | 4709 ± 3397 | 12,008 ± 5586 |
| (−)-Metoprolol | 106 ± 48 | 6358 ± 5857 | 6050 ± 1562 |
| Nadolol | 138 ± 39 | 110 ± 55 | 539 ± 61 |
| (±)-Bupranolol | 50 ± 22 | 5.2 ± 1.7 | 170 ± 89 |
| Carvedilol | 0.3 ± 0.2 | 0.13 ± 0.10 | 0.4 ± 0.1 |
| CGP 20712A | 0.7 ± 0.9 | 4012 ± 2483 | 1960 ± 1189 |
Values are means ± S.D. of three experiments, with each point determined in duplicate.
↵4-a Inhibition of 125I-CYP binding.