Table 2.
AR Binding affinity of selected AR agonists described here (human, if not specified; p, pig; r, rat; m, mouse).a,b
| Compound | pKi A1AR | pKi A2AAR | pKi A3AR | |
|---|---|---|---|---|
| 1 | Adenosine | 7.0 | 6.5 | 6.5 |
| 2 | Metrifudil | 7.22 (r) | 7.62 (r) | 7.33, 7.46 (r) |
| 3 | CPA | 8.64, 9.66 (m) | 6.10, 6.09 (m) | 7.37, 6.27 (m) |
| 4 | Trabodenoson | 9.0 | ND | ND |
| 5 | CHA | 8.62 | 5.86 | 7.14 |
| 6 | SDZ WAG994 | 7.64 (p), 7.12 (r) | 4.64 (p), 5.24 (r) | ND |
| 7 | Cl-ENBA | 9.29, 9.70 (m) | 5.87 | 5.89, 5.62 (m) |
| 8 | MRS7469 | 8.67, 9.43 (m) | 5.45 | 4.97, 6.05 (m) |
| 10 | GS 9667 | 7.92 | <5 | <6 |
| 11 | GR79236X | 8.51 (r) | 5.89 (r) | ND |
| 13 | Tecadenoson | 8.52 | ND | ND |
| 14 | Selodenoson | 8.22 | ND | ND |
| 15 | NNC 21-0136 | 8.33 (r) | 5.89 (r) | ND |
| 16 | MRS5474 | 7.30 | 5.40 | 6.33 |
| 17 | Capadenoson | 8.85 | <5 | <5 |
| 18c | Neladenoson | 10.0 | 6.17 | <5.52 |
| 20 | MMPD | 9.31, 9.68 (r) | 7.15, 7.28 (r) | <5 |
| 21 | Regadenoson | <5, 8.11 (m) | 6.34, 7.11 (m) | <5, <5 (m) |
| 22 | BVT.115959 | 6.81 | 6.01 | 6.81 |
| 23 | Sonedenson | <5 | 6.31 | ND |
| 24 | Binodenoson | 4.32 | 6.57 | <4 |
| 25 | Apadenson | 7.11 | 9.30 | 7.35 |
| 26 | Evodenoson | 7.24 | 9.15 | 6.60 |
| 27c | UK-371104 | 6.99 | 7.70 | <6 |
| 28 | UK-432097 | ND | 8.40 | ND |
| 29 | GW328276X | 6.05 | 8.63 | 8.38 |
| 30 | Bay 60-6583 | 6.41, 6.45 (m) | <5, <5 (m) | 6.94, 6.87 (m) |
| 31 | Piclodenoson | 7.29, 7.79 (m) | 5.50, 5.54 (m) | 8.74, 9.66 (m) |
| 32 | Namodenoson | 6.66 | 5.27 | 8.85 |
| 33 | LJ-529 | 6.71 | 6.65 | 9.42 |
| 34 | CP-532,903 | 6.05 (m) | <5 (m) | 8.05 (m) |
| 35 | CP-608,039 | 5.14 | <4.3 | 8.24 |
| 36 | MRS5698 | <5 | <5 | 8.52 |
| 37 | MRS5980 | <5 | <5 | 9.15 |
aReferences: Knutsen et al., 1999; Gao et al., 2003; Kiesman et al., 2009; Alnouri et al., 2015; Meibom et al., 2017; Baraldi et al., 2018; Jacobson et al., 2018; Tosh et al., 2019. bA2BAR affinity (pKi; h, unless noted): 1, 4.8; 18, 7.10 (pEC50); 21, <5; 23, <5; 25, <6; 26, <6; 27, 5.36 (pEC50); 29, 8.30; 30, 6.94, 7.00 (r), 6.87 (m); 31, 4.96; 34, <5 (m). cpEC50 in cAMP assays. ND, not determined.