Table 4. Human β1- and β2-Adrenoceptor Binding Affinity and Receptor Selectivity of 1-(2-(3-(4-(2-(Alkyloxy)ethoxy)phenoxy)-2-hydroxypropylamino)ethyl)-3-((4-hydroxy)phenyl)ureas 28a–ca.
compd | R1 | log KD β1 | n | log KD β2 | n | selectivity ratio (β1/β2) |
---|---|---|---|---|---|---|
19 | –7.49 ± 0.03 | 11 | b | 11 | ||
29a | cyclopentyl | –8.13 ± 0.05 | 12 | –5.45 ± 0.07 | 7 | 478 |
29b | p-FC6H4CH2CH2 | –8.50 ± 0.05 | 9 | –5.91 ± 0.05 | 9 | 389 |
29c | CH3CH2 | –7.04 ± 0.04 | 16 | b | 16 |
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.
Incomplete inhibition of specific 3H-CGP12177 binding meant that generation of an affinity value (log KD value) by this method was not possible.