Table 1.
Summary of pharmacological properties of β2AR ligands
| Ligand | Chemical structure | G protein activation (cAMP accumulation) |
β-arrestin recruitment |
ERK1/2 activation |
|---|---|---|---|---|
| Isoproterenol |
|
++++ | +++ | ++++ |
| THRX-144877 |
|
++++ | ++++ | ++++ |
| Salbutamol |
|
+++ | ++ | +++ |
| Salmeterol |
|
+++ | ++ | +++ |
| Propranolol |
|
– | 0 | + |
| Pindolol |
|
+ | + | ++ |
| Carazolol |
|
– | 0 | + |
| ICI-118551 |
|
– | 0 | – |
| Carvedilol |
|
– | + | + |
Qualitative functional properties of ligands expressed relative to maximal stimulations (++++). Quantitative data, estimation of ligand efficacy and further description can be found in Supplementry Table 2.