Affinities of selected adenosine receptor agonists
| Ki or EC50 (nM)a | |||||
|---|---|---|---|---|---|
| A1 | A2A | A2Bb | A3 | ||
| Nonselective Agonists | |||||
| 1 | Adenosinec | ca. 100 (h) 73 (r) | 310 (h) 150 (r) | 15,000 (h) 5,100 (r) | 290 (h) 6,500 (r) |
| 6 | NECA | 14 (h) 5.1 (r) 2.49 (m) | 20 (h) 9.7 (r) 43.4 (m) | 1,890 (h) 1,110 (r) 656 (m) | 25 (h) 113 (r) 13.2 (m) |
| A1AR-Selective Agonists | |||||
| 7 | CCPA | 0.83 (h) 1.3 (r) 0.269 (m) | 2270 (h) 950 (r) 988 (m) | 18,800 (h) 6,160 (r) 25.300 (m) | 38 (h) 237 (r) 15.6 (m) |
| 8 | 2′-MeCCPA | 3.3 (h) | 9,580 (h) | 37.600 (h) | 1.150 (h) |
| 9 | (S)-ENBA | n.d. (h) 0.34 (r) | n.d. (h) 477 (r) | n.d. | 282 (h) 915 (r) |
| A2AAR-Selective Agonists | |||||
| 10 | CGS21680 | 289 (h) 1800 (r) 961 (m) | 27 (h) 19 (r) 13.7 (m) | >10,000 (h) >10,000 (r) >10,000 (m) | 67 (h) 584 (r) 93.0 (m) |
| 11 | UK-432,097 | n.d. | 4 | n.d. | n.d. |
| 12 | PSB-0777 | 541 (h) ≥10,000 (r) | 360 (h) 44.4 (r) | >10,000 (h) | >10,000 (h) |
| 2 | Regadenoson | >10,000 (h) | 290 (h) | >10,000 (h) | >10,000 (h) |
| A2BAR-Selective (Partial) Agonist | |||||
| 13 | BAY 60-6583 | 387 (h) 514 (r) 351 (m) | >10,000 (h) >10,000 (r) >10,000 (m) | 3–10 (h, EC50) 114 (h) 100 (r) 136 (m) | 223 (h) 2,750 (r) 3,920 (m) |
| A3AR-Selective Agonists | |||||
| 14 | Cl-IB-MECA (CF102, Namodenoson) | 220 (h) 280 (r) 35 (m) | 5360 (h) 470 (r) 290 (m) | >10,000 (h) 1,210 (r) 44,300 (m) | 1.4 (h) 0.33 (r) 0.18 (m) |
| 15 | HEMADO | 330 (h) | 1200 (h) | >30,000 (h) | 1.10 (h) |
| 16 | MRS5698 | >10,000 (h) >10,000 (m) | >10,000 (h) >10,000 (m) | assumed to be inactive | 3.49 (h) 3.08 (m) |
h, human; Ki, inhibition constant; m, mouse; n.d., no data; r, rat.
adata (if available from Ki values from radioligand binding assays) are taken from the literature cited in the text.
bmost A2BAR data are from functional studies (cAMP accumulation).
cadenosine data are from functional studies (cAMP accumulation).