Table 2.
Characterization of the A2AAR agonist, ATL370, by radioligand binding (mean ± SD)
| Receptor | A1AR | A2AAR - higha | A2AAR- lowa | A2BAR | A3AR |
|---|---|---|---|---|---|
| Radioligand |
125I-ABA |
125I-APE |
125I-ZM241385 |
125I-ABOPX |
125I-ABA |
| Human (Ki, nM) |
61.1 ± 11.3 |
0.5 ± 0.2 |
3.8 ± 0.7 |
>10,000 |
130.4 ± 44.4 |
| Mouse (Ki, nM) | 65.3 ± 15.8 | N/A | 4.3 ± 2.8 | >10,000 | 84.2 ± 19.2 |
aAgonists are known to bind to two affinity states of G-protein coupled receptors. Low affinity reflects binding to uncoupled receptors. High affinity refers to binding to receptor-G protein complexes.