Table 7. Agonist Responses of Second- and Third-Generation Ligands at the Human β1-, β2-, and β3-Adrenoceptorsa.
β1 |
β2 |
β3 |
|||||||
---|---|---|---|---|---|---|---|---|---|
compd | log EC50 β1 | % isop max | n | β2b | % isop max at 10 μM | n | β3b | % isop max at 10 μM | n |
1 | –8.64 ± 0.04 | 37.1 ± 2.2 | 5 | 10 μM | 15.2 ± 0.7 | 4 | 10 μM | 8.6 ± 0.4 | 4 |
19 | –8.01 ± 0.04 | 33.6 ± 2.4 | 6 | 10 μM | 8.0 ± 1.1 | 7 | 10 μM | 12.5 ± 2.3 | 7 |
29a | –8.44 ± 0.04 | 25.5 ± 1.1 | 5 | 10 μM | 15.3 ± 1.1 | 4 | 10 μM | 4.0 ± 0.6 | 3 |
29b | –8.64 ± 0.04 | 23.8 ± 1.5 | 5 | 10 μM | 16.0 ± 1.3 | 4 | 10 μM | 7.9 ± 0.1 | 4 |
29c | –7.64 ± 0.04 | 35.9 ± 1.7 | 5 | 10 μM | 27.8 ± 2.3 | 3 | 10 μM | 1.3 ± 0.1 | 3 |
37a | –8.35 ± 0.10 | 28.3 ± 1.9 | 5 | 10 μM | 15.3 ± 1.0 | 4 | 10 μM | 4.0 ± 0.3 | 4 |
37l | –8.52 ± 0.08 | 29.1 ± 1.7 | 4 | 10 μM | 12.7 ± 0.7 | 3 | 10 μM | 2.0 ± 0.1 | 3 |
Values represent the mean ± SEM of n separate experiments. Log EC50 values and % isoprenaline maximal responses were obtained from 3H-cAMP accumulation for cells expressing the human β1-adrenoceptor.
For the human β2- and β3-adrenoceptors, the top of the agonist concentration response curve was not obtained even with the maximum concentration of ligand. In these instances, the percentage of isoprenaline response is given for the response at 10 μM of ligand.