Radioligand binding affinity estimates (Ki) of GSK-961081 and comparator drugs determined by displacement of [3H]dihydroalprenolol at β1- or β2-adrenoceptors expressed in HEK293 cell membranes (n = 28–60) or displacement of [125I]cyanopindolol at β3 expressed in CHO-K1 cell membranes (n = 15–45)
Data shown are mean ± S.D.
| Compound | Ki | Selectivity | |||
|---|---|---|---|---|---|
| β1 | β2 | β3 | β1/β2 | β3/β2 | |
| nM | |||||
| GSK-961081 | 456 ± 246 | 3.7 ± 1.4 | 1215 ± 1108 | 123 | 328 |
| Salmeterol | 2585 ± 1047 | 2.7 ± 0.8 | >10,000 | 957 | >3700 |
| Formoterol | 2160 ± 563 | 36.9 ± 15.3 | 1511 ± 1097 | 59 | 41 |
| Albuterol | 7160 ± 1746 | 1663 ± 682 | >10,000 | 4.3 | >6 |
| Isoproterenol | 370 ± 152 | 453 ± 118 | 445 ± 421 | 0.8 | 1 |