Table 2.
Selectivity ratios of the β-blockers for human β1-, β2- and β3-adrenoceptors, where a ratio of 1 demonstrates no selectivity for a given receptor subtype over another
| Selectivity ratios | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| β1 | vs | β2 | β2 | vs | β3 | β1 | vs | β3 | |
| β-ligands | |||||||||
| CGP 20712A | 501.2 | 8.3 | 4168.7 | ||||||
| ICI 89406 | 69.2 | 24.0 | 1659.6 | ||||||
| Practolol | >14.1 | >9.8 | >138.0 | ||||||
| Xamoterol | 14.1 | 41.7 | 588.8 | ||||||
| Bisoprolol | 13.5 | 10.7 | 144.5 | ||||||
| Betaxolol | 6.8 | 25.7 | 173.8 | ||||||
| Atenolol | 4.7 | 75.9 | 354.8 | ||||||
| ICI 215001 | 3.2 | 5.9 | 1.8 | ||||||
| Acebutolol | 2.4 | 46.8 | 112.2 | ||||||
| Metoprolol | 2.3 | 53.7 | 125.9 | ||||||
| CGP 12177 | 1.5 | 251.2 | 166.0 | ||||||
| Labetolol | 2.5 | 70.8 | 28.2 | ||||||
| Carvedilol | 4.5 | 12.6 | 2.8 | ||||||
| Pronethalol | 8.3 | 29.5 | 3.5 | ||||||
| Propranolol | 8.3 | 141.3 | 17.0 | ||||||
| Sotalol | 12.0 | 63.1 | 5.2 | ||||||
| CL 316243 | >12.6 | 10.2 | >128.8 | ||||||
| Alprenolol | 16.2 | 128.8 | 7.9 | ||||||
| Bupranolol | 21.9 | 645.7 | 29.5 | ||||||
| Nadolol | 23.4 | 263.0 | 11.2 | ||||||
| Timolol | 25.7 | 758.6 | 29.5 | ||||||
| ICI 118551 | 549.5 | 660.7 | 1.2 | ||||||
| Clinically-used β-agonists | |||||||||
| Salbutamol | 28.8 | 61.7 | 2.1 | ||||||
| Terbutaline | 63.1 | 52.5 | 1.2 | ||||||
| Salmeterol | 2818.4 | 1258.9 | 2.2 | ||||||
Thus, the affinity of CGP 20712A is 501-fold more at the β1- than β2-receptor.