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. 2013 Apr 24;56(10):3852–3865. doi: 10.1021/jm400348g

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 28aca.

compd R1 log KD β1 n log KD β2 n selectivity ratio (β12)
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  
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.