Table 1.
Ki apparent values for binding of nucleoside monomers and dendrimer conjugates at A1, A2A, and A3 ARs.a
| Compound | A1 Ki (nM) | A2A Ki (nM) | A3 Ki (nM) |
| Nucleoside Monomers | |||
| 1 | 10.4 ± 3.8 | 370 ± 100 | 12.2 ± 4.1 |
| 4d | 30 ± 9 | 800 ± 360 | 74 ± 20 |
| 7d | 43 ± 5 | 300 ± 20 | 9.5 ± 2.0 |
| Dendrimer Derivatives | |||
| 11 | NBb | (20 ± 7%)c | (26 ± 3%)c |
| 12 | 21 ± 5 | 250 ± 40 | 27 ± 2 |
| 13 | 55 ± 10 | 405 ± 170 | 42 ± 17 |
| 15 | NBb | NBb | NBb |
| 16 | 175 ± 60 | 610 ± 110 | 14.0 ± 2.1 |
| 17d | 320 ± 20 | 470 ± 50 | 2.4 ± 0.4 |
a. All experiments were performed using adherent CHO cells stably expressing the A1 or A3 AR or HEK cells stably expressing A2A AR. Binding was carried out as described in methods using [3H]CCPA, [3H]CGS21680, or [125I]AB-MECA. Values are expressed as Ki values (mean ± SEM, n = 3) or as displacement of the radioligand at 10 μM. b. NB, No binding. Inhibition of radioligand binding < 10% at 10 μM. c. Percent inhibition of radioligand binding at 10 μM. d. 4, MRS5145; 7, MRS5169; 17, MRS5183.