TABLE 1.
Binding and functional characteristics of TAP-A2AR receptors in HEK293 cells
Results from cAMP assays were fitted to the equation describing a hyperbola with a constant basal term. Emax refers to the maximum [3H]cAMP accumulation (cpm). Dissociation constants (KD) and the amount of A2A receptors in the selected stably transformed cell clones were calculated by fitting specific binding of the antagonist [3H]ZM241385 to the equation for a rectangular hyperbola.
| Construct | EC50 | Emax | KD | Bmax |
|---|---|---|---|---|
| nm | cpm | nm | pmol/mg | |
| G2S-N-hA2AR-4 | 5.2 ± 1.2 | 2354 ± 75 | 2.0 ± 0.7 | 6.8 ± 0.7 |
| G2S-N-hA2AR-8 | 3.6 ± 1.6 | 958 ± 92 | 2.6 ± 0.5 | 3.0 ± 0.2 |
| G2S-N-hA2AR-9 | 5.1 ± 1.8 | 1804 ± 221 | 2.1 ± 0.3 | 2.5 ± 0.01 |
| G2S-C-hA2AR-1 | 109 ± 1.6 | 2623 ± 346 | 4.2 ± 1.1 | 0.9 ± 0.1 |
| G2S-C-hA2AR-5 | 170 ± 1.4 | 3504 ± 358 | 4.5 ± 2.0 | 1.4 ± 0.2 |
| G2S-C-hA2AR-6 | 140 ± 1.5 | 2276 ± 273 | 4.0 ± 0.8 | 1.0 ± 0.1 |
| FS2-N-hA2AR-5 | 2.9 ± 1.6 | 3358 ± 251 | 2.6 ± 1.1 | 14.5 ± 2.0 |
| FS2-N-hA2AR-7 | 5.6 ± 1.1 | 4484 ± 166 | 1.3 ± 0.1 | 7.0 ± 0.3 |
| FS2-N-hA2AR-10 | 6.8 ± 1.6 | 3182 ± 219 | 2.4 ± 0.9 | 11.5 ± 1.3 |