Log EC50 values and percentage of isoprenaline maximum values for a range of β-ligands when measured at both [3H]cAMP accumulation and CRE-luciferase production in CHO-β3 cells Values given are mean ± S.E.M. of n determinations. Ligands with agonist activity at high concentrations (top of response not reached by 100 μM) include acebutolol, dopamine, ephedrine, ICI 89406, nadolol, and procaterol. Ligands with no intrinsic efficacy include atenolol, betaxolol, bisoprolol, bupranolol, CGP 20712A, ICI 118551, metoprolol, practolol, and sotalol.
| Ligand | [3H]cAMP Accumulation | CRE-Luciferase Production | ||||
|---|---|---|---|---|---|---|
| Log EC50 | % Isoprenaline | n | Log EC50 | % Isoprenaline | n | |
| Fenoterol | –7.56 ± 0.05 | 98.5 ± 1.0 | 4 | –7.56 ± 0.03 | 102.6 ± 1.6 | 14 |
| Terbutaline | –5.53 ± 0.06 | 97.5 ± 1.4 | 6 | –5.68 ± 0.13 | 110.6 ± 3.0 | 4 |
| Salbutamol | –5.76 ± 0.08 | 88.8 ± 3.0 | 4 | –5.76 ± 0.12 | 108.2 ± 2.0 | 4 |
| Tulobuterol | –5.40 ± 0.05 | 76.6 ± 4.6 | 5 | –5.40 ± 0.12 | 107.7 ± 3.5 | 4 |
| Cimaterol | –6.73 ± 0.08 | 86.2 ± 2.5 | 6 | –6.71 ± 0.04 | 106.3 ± 1.8 | 7 |
| BRL 37344 | –7.38 ± 0.05 | 79.2 ± 3.4 | 4 | –7.52 ± 0.03 | 98.4 ± 1.7 | 13 |
| Pronethalol | –5.34 ± 0.07 | 7.8 ± 3.7 | 9 | –4.82 ± 0.16 | 24.2 ± 11.0 | 3 |
| ICI 215001 | –7.06 ± 0.06 | 60.3 ± 2.9 | 5 | –7.27 ± 0.03 | 89.2 ± 2.8 | 6 |
| Clenbuterol | –5.90 ± 0.07 | 77.7 ± 2.8 | 4 | –5.91 ± 0.10 | 109.3 ± 2.2 | 4 |
| Dobutamine | –6.27 ± 0.01 | 87.3 ± 1.6 | 5 | –6.29 ± 0.08 | 106.9 ± 3.4 | 4 |
| CL 316243 | –6.03 ± 0.04 | 75.8 ± 4.5 | 6 | –6.17 ± 0.12 | 99.8 ± 3.8 | 4 |
| Salmeterol | –6.23 ± 0.07 | 84.2 ± 2.5 | 5 | –6.15 ± 0.07 | 139.2 ± 1.9 | 4 |
| Formoterol | –7.72 ± 0.08 | 99.6 ± 3.5 | 4 | –7.72 ± 0.10 | 113.0 ± 2.8 | 4 |
| Noradrenaline | –7.14 ± 0.07 | 96.9 ± 2.2 | 6 | –7.29 ± 0.04 | 106.9 ± 2.1 | 8 |
| Adrenaline | –6.55 ± 0.06 | 96.5 ± 1.8 | 5 | –6.67 ± 0.04 | 109.5 ± 2.1 | 7 |
| Isoprenaline | –7.35 ± 0.05 | 100 | 5 | –7.48 ± 0.05 | 100 | 15 |
| Labetolol | –5.32 ± 0.06 | 9.8 ± 0.5 | 10 | –4.97 ± 0.09 | 37.4 ± 2.1 | 5 |
| Pindolol | –5.67 ± 0.06 | 39.3 ± 1.0 | 8 | –5.69 ± 0.05 | 90.1 ± 4.0 | 8 |
| CGP 12177 | –6.57 ± 0.09 | 61.4 ± 1.5 | 6 | –6.93 ± 0.03 | 101.7 ± 1.4 | 15 |
| SR 59230A | –7.21 ± 0.04 | 12.3 ± 0.8 | 9 | –6.49 ± 0.06 | 37.5 ± 5.7 | 10 |
| Alprenolol | –5.69 ± 0.07 | 17.5 ± 1.3 | 6 | –5.56 ± 0.09 | 54.1 ± 5.5 | 10 |
| Carvedilol | –7.19 ± 0.22 | 8.0 ± 0.5 | 9 | –6.10 ± 0.12 | 44.9 ± 6.5 | 6 |
| Propanolol | –5.49 ± 0.10 | 7.5 ± 0.5 | 12 | –5.10 ± 0.10 | 23.1 ± 7.1 | 3 |
| Timolol | –5.55 ± 0.14 | 5.7 ± 0.5 | 6 | –4.77 ± 0.07 | 20.4 ± 11.5 | 3 |