Table 6. Antagonist Affinities for Second- and Third-Generation Ligands at the Human β1-, β2-, and β3-Adrenoceptorsa.
| compd | log KD β1 | n | log KDβ2 | n | log KDβ3 | n | selectivity β1 vs β2 |
|---|---|---|---|---|---|---|---|
| 19 | –7.75 ± 0.06 | 21 | –5.15 ± 0.06 | 7 | >10 μM | 7 | 398 |
| 29a | –8.55 ± 0.04 | 12 | –5.84 ± 0.06 | 4 | >10 μM | 4 | 513 |
| 29b | –9.00 ± 0.04 | 9 | –6.05 ± 0.05 | 4 | –5.58 ± 0.09 | 4 | 891 |
| 29c | –7.57 ± 0.05 | 12 | >10 μM | 4 | >10 μM | 4 | >372 |
| 37a | –8.46 ± 0.05 | 12 | –5.92 ± 0.02 | 4 | >10 μM | 4 | 347 |
| 37l | –8.83 ± 0.06 | 9 | –6.10 ± 0.10 | 4 | –5.22 ± 0.08 | 4 | 537 |
a
Values represent the mean ± SEM of n separate experiments. Log KD values were obtained from 3H-cAMP accumulation assays following inhibition of the cimaterol agonist response in CHO cells stably expressing the human β1-, β2-, or β3-adrenoceptors.