TABLE 1.
pEC50 ± SD | Maximum | ||||||||
---|---|---|---|---|---|---|---|---|---|
Assay | WT | F193A | Shift | Significant | WT (%) | F193A (%WT) | Significant | SI (%) | |
Arrestin BRET | 7.71 ± 0.29 | 5.26 ± 0.11 | 2.45 | Y | 100 | 56.4 ± 4.7 | Y | 60.8 | |
cAMP | 7.92 ± 0.47 | 7.86 ± 0.41 | 0.06 | N | 100 | 111.9 ± 4.1 | N | 98.4 | |
mGs BRET | 7.98 ± 0.55 | 6.67 ± 0.26 | 1.31 | Y | 100 | 102.2 ± 9.6 | N | 99.9 |
Comparison of Wild-type β2-adrenergic receptor (β2AR-WT) and β2AR-F193A across assays. Negative log of the half-maximal effective concentration (pEC50) values and maximum response relative to β2AR-WT are listed. Shift indicates the difference in pEC50 values for β2AR-WT and β2AR-F193A. Significance for pEC50 and maximum response was determined by t test for n = 3 experiments. Stimulus inactivation indicates a comparison of agonist doses that promote equal response in WT and mutant receptor in each assay. This parameter was estimated as described previously (Ostrom and Ehlert, 1997). Briefly, equiactive isoproterenol concentrations were compared between β2AR-WT and β2AR-F193A by interpolating equivalent β2AR-F193A responses from β2AR-WT dose response curves. The stimulus inactivation (SI) parameter denotes the apparent efficacy of β2AR-F193A compared with wild-type.