Characterization of CHO cells expressing WT and mutated α2-ARs.
| Cell line | [3H]RX821002 | CEC | ||
|---|---|---|---|---|
| Bmax | Kd | nH | ApparentKi | |
| fmol/mg of protein | nm | nm | ||
| CHO-Hα2Awt (Cys201) | 595 ± 2 | 0.60 ± 0.02 | 0.98 ± 0.02 | 578 ± 39 |
| CHO-Hα2ASer201 | 156 ± 13 | 0.30 ± 0.04 | 0.95 ± 0.06 | 260 ± 32 |
| CHO-Hα2ASer201Cys197 | 295 ± 22 | 0.53 ± 0.05 | 1.02 ± 0.07 | 95 ± 3 |
| CHO-Hα2ASer201Cys198 | 3710 ± 120 | 0.72 ± 0.09 | 0.98 ± 0.02 | 467 ± 49 |
| CHO-Hα2ASer201Cys199 | 10967 ± 260 | 1.90 ± 0.11 | 0.95 ± 0.01 | 2624 ± 96 |
| CHO-Hα2ASer201Cys200 | 2146 ± 306 | 3.34 ± 0.51 | 0.99 ± 0.01 | 56 ± 6 |
| CHO-Hα2ASer201Cys204 | 4009 ± 117 | 2.71 ± 0.12 | 1.00 ± 0.01 | 191 ± 7 |
| CHO-Hα2Bwt | 1870 ± 111 | 6.12 ± 0.46 | 1.00 ± 0.01 | 1016 ± 115 |
| CHO-Hα2Cwt | 1324 ± 251 | 1.18 ± 0.17 | 0.96 ± 0.04 | 2909 ± 4 |
| CHO-Mα2Awt | 1707 ± 164 | 0.89 ± 0.09 | 0.92 ± 0.05 | 539 ± 46 |
| CHO-Mα2ACys201 | 1803 ± 143 | 1.26 ± 0.14 | 0.98 ± 0.01 | 1484 ± 223 |
The concentration of CEC that inhibited specific [3H]RX821002 binding in competition assays by 50% (IC50) was used to calculate apparent Ki values (inhibition constant) according to the Cheng-Prusoff equation.
CHO, Chinese hamster ovary.