125I-CYP | Salmeterol,Ki | ||
---|---|---|---|
Kd | Bmax | ||
pm | pmol/mg of protein | nm | |
WT β2AR | 23.2 ± 3.1 | 4.4 ± 0.4 | 1.5 ± 0.4 |
CH-1 | 56.1 ± 0.6 | 4.4 ± 0.1 | 18 ± 4 |
CH-2 | 15.8 ± 0.8 | 4.9 ± 0.01 | 49 ± 1 |
CH-3 | 47.3 ± 3.6 | 23.6 ± 1.4 | 2,800 ± 2901-a |
CH-4 | 142 ± 141-a | 54.5 ± 5.9 | 1,300 ± 1201-b |
CH-5 | 54.1 ± 3.2 | 28.3 ± 0.3 | 3,100 ± 4101-a |
CH-6 | 66.7 ± 11.01-b | 6.6 ± 0.3 | 10,000 ± 690a,c |
CH-7 | 129 ± 24a,c | 2.2 ± 0.7 | 270 ± 681-c |
CH-8 | 40.6 ± 2.2 | 0.2 ± 0.1 | 25 ± 71-c |
WT β1AR | 36.9 ± 5.2 | 19.9 ± 5.6 | 2,200 ± 79 |
The binding of salmeterol to the WT β1- and β2ARs and β1/β2 chimeric receptors was assayed by competition with 50 pm125I-CYP. The data were analyzed by a nonlinear least-squares regression computer program, as described in Experimental Procedures. The results are shown as the mean ± standard error of three or four separate experiments.