Affinity and selectivity values of selected A3AR agonists
Affinity values are derived from Fredholm et al., 2011, unless otherwise indicated.
| A3AR Agonists | A1AR Ki | A2AAR Ki | A2BAR Ki | A3AR Ki | A1/A3 | A2A/A3 |
|---|---|---|---|---|---|---|
| nM | ||||||
| IB-MECA (CF101) | 51 (h) | 2900 (h) | 11,000 (h) | 1.8 (h) | 28 | 1611 |
| Cl-IB-MECA (CF 102) | 220 (h) | 5360 (h) | >10,000 (h) | 1.4 (h) | 157 | 3829 |
| 280 (r) | 470 (r) | >10,000 (m) | 0.33 (r) | 848 | 1424 | |
| 35 (m) | ≈10,000 (m) | N.D. | 0.18 (m) | 194 | >55,000 | |
| LJ529 | 193 (h)a | 223 (h)a | N.D. | 0.38 (h)a | 508 | 586 |
| PEMADO | 32,800 (h) | 41,700 (h) | >30,000 (h) | 0.44 (h) | 74,545 | 94,773 |
| HEMADO | 330 (h) | 1200 (h) | >30,000 (h) | 1.10 (h) | 300 | 1091 |
| CP608,039 | 7300 (h) | >50,000 (h) | N.D. | 5.8 (h) | 1259 | >8621 |
| 1750 (rb) | N.D. | N.D. | 83 (rb) | 21 | N.D. | |
| MRS3558 (CF502) | 260 (h) | 2330 (h) | >10,000 (h) | 0.29 (h) | 897 | 8034 |
| 105 (r) | 1080 (r) | N.D. | 1.0 (r) | 105 | 1080 | |
| 15.8 (m) | 10,400 (m) | N.D. | 1.49 (m) | 11 | 6980 | |
| MRS5151 | 14,900 (h) | ≈10,000 (h) | N.D. | 2.38 (h) | 6261 | >4200 |
| 10,500 (m) | >10,000 (m) | N.D. | 24.4 (m) | 430 | >410 | |
h, human; m, mouse; r, rat; rb, rabbit; N.D., no data available.
↵a Values are derived from Baraldi et al., 2012.