[3H]CGP 12177 whole-cell binding in transiently transfected cell populations
The measure of duration of binding is the log shift of the curve from the control curve to the duration curve run in parallel in each experiment. The log KD values for carvedilol are also given. The values are mean ± S.E.M. for n separate experiments, and each separate n number has been obtained in a separate transiently transfected population of cells. Thus, salbutamol is short-acting in that the IC50 of the binding curve is shifted more than 2 log units (100-fold) to the right following washout at all receptors. Carvedilol, however, is long-acting as the duration curve remains in a similar place to the control curve (and the shift in IC50 is about 0).
| Salmeterol | Salbutamol | Formoterol | Fenoterol | Carvedilol | |||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Shift (log) | n | Shift (log) | n | Shift (log) | n | Shift (log) | n | Log KD | Shift (log) | n | |
| β1-WT | 0.86 ± 0.08 | 4 | >2 | 4 | >2 | 4 | >2 | 4 | −9.01 ± 0.12 | 0.26 ± 0.08 | 4 |
| β2-WT | 0.52 ± 0.14 | 5 | >2 | 5 | 1.96 ± 0.12 | 5 | 2.65 ± 0.14 | 5 | −9.62 ± 0.09 | −0.03 ± 0.10 | 5 |
| β2-EL3 | 0.84 ± 0.11 | 5 | >2 | 5 | 1.75 ± 0.14 | 5 | 2.56 ± 0.05 | 5 | −9.33 ± 0.01 | −0.10 ± 0.06 | 5 |
| β2-F194V | 0.80 ± 0.08 | 5 | >2 | 5 | 2.07 ± 0.08 | 5 | 2.68 ± 0.05 | 4 | −9.61 ± 0.08 | −0.12 ± 0.09 | 5 |
| β2-H296K | 0.57 ± 0.13 | 5 | >2 | 5 | 1.70 ± 0.20 | 5 | 2.49 ± 0.08 | 5 | −9.20 ± 0.11 | −0.42 ± 0.02 | 5 |
| β2-R304P | 0.51 ± 0.10 | 4 | >2 | 4 | 1.78 ± 0.18 | 4 | 2.53 ± 0.17 | 4 | −9.48 ± 0.16 | 0.11 ± 0.08 | 4 |
| β2-K305D | 0.91 ± 0.07 | 5 | >2 | 5 | 2.06 ± 0.08 | 5 | 2.48 ± 0.14 | 5 | −9.42 ± 0.09 | 0.27 ± 0.10 | 5 |
| β2-Y308F | 0.78 ± 0.04 | 4 | >2 | 4 | 2.28 ± 0.13 | 4 | >2 | 4 | −9.61 ± 0.07 | 0.13 ± 0.13 | 4 |
| β2-F194V-K305D | 1.07 ± 0.05 | 5 | >2 | 5 | 2.30 ± 0.15 | 5 | 2.65 ± 0.07 | 5 | −9.62 ± 0.12 | 0.17 ± 0.07 | 5 |
| β2-R304P-K305D | 0.91 ± 0.04 | 4 | >2 | 4 | 2.10 ± 0.14 | 4 | 2.47 ± 0.10 | 4 | −9.34 ± 0.07 | 0.08 ± 0.16 | 4 |
| β2-H296K-Y308F | 0.88 ± 0.13 | 5 | >2 | 5 | 1.60 ± 0.19 | 5 | >2 | 5 | −9.47 ± 0.06 | −0.31 ± 0.18 | 5 |
| β2-K305D-Y308F | 0.67 ± 0.09 | 5 | >2 | 5 | 1.96 ± 0.21 | 4 | >2 | 5 | −9.62 ± 0.07 | 0.16 ± 0.11 | 4 |
| β2-H296K-K305D | 0.67 ± 0.09 | 5 | >2 | 5 | 1.43 ± 0.16 | 5 | 2.07 ± 0.19 | 5 | −9.39 ± 0.12 | −0.43 ± 0.14 | 5 |