Table 2.
Percent inhibition of radioligand binding or binding affinities of apioadenosine derivatives at three hAR subtypes.a
| Compound | A1 AR, % inhibition | A2A AR, % inhibition | A3 AR, % inhibition or Ki (nM) |
|---|---|---|---|
| 4 | 6 ± 4% | 19±8% | 35 ± 4% |
| 5 | 6 ± 5% | 19±10% | 32 ± 2% |
| 6 | 10 ± 7% | 15±12% | 31 ± 2% |
| 7 | 0% b | 64% b | 10% |
| 8 | 74% b | 76% b | 7% |
| 9 | 0% b | ND | 7% |
| 10a | 10 ± 6% | 10±8% | 43 ± 5% |
| 10b | 27 ± 9% | 17±11% | 48 ± 6% |
| 10c | 12 ± 3% | 17±6% | 978 ± 175 |
| 11a | 19 ± 1% | 15 ± 5% | 44 ± 1% |
| 11b | 35 ± 5% | 22 ± 2% | 45 ± 1% |
| 11c | 13 ± 5% | 14 ± 5% | 3070 ± 750 |
| 12 | 12 ± 4% | 10±8% | 26 ± 6% |
| 13 | 9 ± 5% | 12 ± 4% | 6 ± 2% |
| 14 | 7 ± 2% | 2 ± 2% | 8 ± 1% |
| 15 | 8 ± 7% | 9 ± 5% | 10 ± 2% |
| 16 | 6 ± 5% | 12 ± 7% | 3 ± 2% |
a
Binding in membranes of CHO or HEK293 (A2AR only) cells stably expressing one of three hAR subtypes. Percent refers to inhibition of binding at 10 μM, unless noted, using agonists [3H]N6-[(R)-1-methyl-2-phenylethyl]adenosine, [3H]2-[p-(2-carboxyethyl)phenylethylamino]-5′-N-ethylcarboxamidoadenosine, or [125I]N6-(4-amino-3-iodobenzyl)adenosine-5′-N-methyluronamide, respectively. Values not in italics refer to the binding affinity at hA3ARs expressed as a Ki value. Values are mean ± S.E.M.
b
Percent refers to inhibition of binding at 50 μM. ND, not determined.