Table 1. Human β1- and β2-Adrenoceptor Binding Affinities for Established β-Adrenoceptor Ligands, 1 and 19a.
| compd | log KD β1 | n | log KD β2 | n | selectivity ratio (β1/β2) |
|---|---|---|---|---|---|
| CGP 20712A | –8.79 ± 0.07 | 9 | –5.82 ± 0.04 | 8 | 933 |
| ICI 118551 | –6.62 ± 0.01 | 9 | –9.17 ± 0.03 | 8 | 354 β2 selective |
| xamoterol | –7.09 ± 0.04 | 8 | –5.76 ± 0.04 | 8 | 21 |
| ICI 89406 | –8.75 ± 0.03 | 9 | –6.84 ± 0.03 | 9 | 81 |
| 1 | –8.04 ± 0.03 | 9 | –5.29 ± 0.04 | 11 | 562 |
| 19 | –7.49 ± 0.03 | 11 | b | 11 |
a
Values represent the mean ± SEM of n separate experiments. Log KD values were obtained from 3H-CGP 12177 whole cell binding studies in CHO cells stably expressing the human β1 or β2-adrenoceptors.
b
Incomplete inhibition of specific 3H-CGP12177 binding meant that generation of an affinity value (log KD value) by this method was not possible.