Table 4.
Covalent ligands for adenosine receptors
| Ligands | Apparent IC50/Ki/KD (nM)a | Functionality | Ref | ||||
|---|---|---|---|---|---|---|---|
| A1 | A2A | A2B | A3 | ||||
| A1 | 125I-APNEA | 2.0 (r) | N.D. | N.D. | N.D. | Agonist | [113] |
| R-AHPIA | 1.6 (r) | N.D. | N.D. | N.D. | Agonist | [113] | |
| 125I-AHPIA | 2.0 (r) | N.D. | N.D. | N.D. | Agonist | [113] | |
| 125I-azido-BW-A844U | 0.14 (b) | N.D. | N.D. | N.D. | Antagonist | [114] | |
| p-DITC-ADAC | 0.47 (r) | 191 (r) | N.D. | N.D. | Agonist | [115] | |
| m-DITC-ADAC | 0.87 (r) | 176 (r) | N.D. | N.D. | Agonist | [115] | |
| LUF7746 | 4.0 | 26% (1 μM) | 26% (1 μM) | 25% (1 μM) | Partial agonist | [116] | |
| m-DITC-XAC | 2.4 (r) | 343 (r) | N.D. | N.D. | Antagonist | [115] | |
| FSCPX | 12 | 1200 | N.D. | N.D. | Antagonist | [117] | |
| DU172 | 21 | 2.8 | N.D. | N.D. | Antagonist | [117] | |
| A2A | 125I-azido-PAPA-APEC | N.D. | 1.2 | N.D. | N.D. | Agonist | [118] |
| [125I]AzPE | N.D. | 1.7 | N.D. | N.D. | Agonist | [119] | |
| “9” | N.D. | 40 | N.D. | N.D. | Agonist | [120] | |
| p-DITC-APEC | 276 (r) | 35 (r) | N.D. | N.D. | Agonist | [121] | |
| MRS5854 | 500 | 23 | N.D. | 207 | Agonist | [122] | |
| MRS5854-azide | 30% (10 μM) | 4360 | N.D. | 1810 | Agonist | [122] | |
| ISC | 20,300 | 111 | N.D. | Antagonist | [123] | ||
| LUF7445 | 372 | 1.0 | 0% (1 μM) | 49 | Antagonist | [124] | |
| LUF7487 | 19 | 1.5 | N.D. | 60 | Antagonist | [6] | |
| A3 | MRS1163 | 145 (r) | 272 (r) | N.D. | 10.0 (r) | Agonist | [125] |
| SO2F-MRS1191 | 41% (100 μM, r) | 20% (100 μM, r) | N.D. | 2.4 | Antagonist | [126] | |
| SO2F-MRE-3008-F20 | < 5% (100 nM) | 50 | N.D. | 79% (100 nM) | Antagonist | [127] | |
| LUF7602 | 794 | 1300 | 0% (10 μM) | 10 | Antagonist | [128] | |
N.D. not determined
aThe data are apparent affinities (nM) for the human adenosine receptors or % displacement at the concentration in brackets unless indicated otherwise (r = rat, b = bovine)