Affinities of agonists and antagonists for wild-type and N293D mutant β2-adrenergic receptors
| Affinity (Ki) | ||
|---|---|---|
| Wild-type | N293D | |
| nM | ||
| (−)-Isoproterenol | 280 ± 76 | 5760 ± 460 |
| (+)-Isoproterenol | 280 ± 76 | 5760 ± 460 |
| (+)-Isoproterenol | 10,600 ± 2,390 | 87,500 ± 11,000 |
| (−)-Epinephrine | 1,450 ± 50 | 38,600 ± 10,000 |
| (±)-Terbutaline | 10,900 ± 5,400 | 51,900 ± 12,900 |
| (±)-Dobutamine | 66,000 ± 21,000 | 80,000 ± 39,000 |
| (−)-Alprenolol | 2.1 ± 0.4 | 2.4 ± 0.4 |
| (−)-Propranolol | 1.04 ± 0.28 | 0.86 ± 0.02 |
| (+)-Propranolol | 108 ± 30 | 66 ± 14 |
| ICI118,551 | 0.32 ± 0.04 | 0.82 ± 0.13 |
The affinities were determined in competition experiments with 30 nM125I-CYP in the presence of 100 μM GTP and were calculated by nonlinear regression. Data are means ± SEM, n = 3.