Binding affinity of β 1-adrenoceptor mutants for [3H]dihydroalprenolol
| X Labels | Kd | Bmax | ||||
|---|---|---|---|---|---|---|
| Mean | S.E.M. | n | Mean | S.E.M. | n | |
| nM | fmol/mg | |||||
| WT-β1-AR | 0.77 | 0.18 | 3 | 822 | 152 | 3 |
| L322K-β1-AR | 1.34 | 0.04 | 3 | 1603 | 215 | 3 |
| CAM-β1-AR | 1.46 | 0.21 | 3 | 2997 | 445 | 3 |
| CAMK-β1-AR | 1.36 | 0.24 | 3 | 385 | 41 | 3 |
| R156A-β1-AR | 1.28 | 0.23 | 4 | 4330 | 311 | 4 |
The binding affinity for [3H]dihydroalprenolol and steady-state levels of expression of the various forms of the β1-adrenoceptor were assessed in saturation ligand binding studies. Such studies allowed membrane amounts corresponding to 10 fmol of each construct to be added to [35S]GTPγ S binding assays.