Comparison of high- and low-affinity K i values for selected agonist compounds at the hA2AAR
| Low Affinity (Ki,L) | n | High Affinity (Ki,H) | n | Low/High | |
|---|---|---|---|---|---|
| nM | nM | ||||
| ATL 146e | 67.9 ± 10 | 4 | 0.20 ± 0.02 | 6 | 340 |
| [125I]APE | 26 ± 6 | 3 | 0.46 ± 0.1 | 3 | 57 |
| CGS 21680 | 944 ± 200 | 3 | 4.9 ± 0.20 | 5 | 192 |
| NECA | 84.7 ± 38 | 5 | 2.0 ± 0.20 | 4 | 42 |
| IB-MECA | 5,429 ± 1,070 | 3 | 6.3 ± 0.80 | 3 | 862 |
| CI-IBMECA | 7,692 ± 980 | 3 | 18.3 ± 3.2 | 4 | 420 |
| CCPA | 5,466 ± 293 | 3 | 11.0 ± 1.9 | 4 | 497 |
| CPA | 10,370 ± 350 | 3 | 19.8 ± 3.2 | 4 | 523 |
K iL (expressed as mean ± S.E.M.) values were determined from the IC50 of the agonist in competition with125I-ZM241285 on A2A receptors expressed in Sf9 cells. High-affinity K iH values were determined from the IC50 of the drug in competition with [125I]APE on A2A receptors expressed with heterotrimeric G proteins (αs,β4,γ2) in Sf9 cells.
n, number of independent experiments done in triplicate.