Table 1.
Adenosine receptor affinities of agonists.
| Ki (nM)a
|
|||||
|---|---|---|---|---|---|
| A1 | A2A | A2Bb | A3 | ||
| 1 | Adenosinec [35] | ca. 100 (h) | 310 (h) | 15,000 (h) | 290 (h) |
| 73 (r) | 150 (r) | 5100 (r) | 6500 (r) | ||
| A1-selective agonists | |||||
| 2 | R-PIA | 2.04 (h) [128] | 220 (r) [129] | 150,000 (h) [130] | 33 (h) [132] |
| 1.2 (r) [129] | 158 (r) [133] | ||||
| 19,000 (m) [131] | |||||
| 3 | CPA [109] | 2.3 (h) | 794 (h) | 18,600 (h) | 72 (h) |
| 4 | CCPA | 0.83 (h) [109] | 2270 (h) [109] | 18,800 (h) [109] | 38 (h) [109] |
| 1.3 (r) [134] | 950 (r) [134] | 237 (r) [134] | |||
| 0.1 (rb) [134] | 37.7 (rb) [134] | ||||
| 5 | (S)-ENBA [19] | 0.34 (r) | 477 (r) | ndd | 282 (h) |
| 915 (r) | |||||
| 6 | Capadenoson (BAY68-4986) | nd | nd | nd | nd |
| 7 | GW493838 | nd | nd | nd | nd |
| 8 | Selodenoson (DTI-0009) | nd | nd | nd | nd |
| 9 | GR79236 [109] | 3.1 (r) | 1300 (h) | nd | nd |
| 10 | Tecadenoson [109] | 6.5 (p) | 2315 (h) | nd | nd |
| 11 | CVT-3619 (GS 9667) [135] | 55 (h) | > 10,000 (h) | >50,000 (h) | > 1000 (h) |
| 12 | AMP579 [136] | 5.0 (r) | 56 (r) | nd | nd |
| 13 | SDZ WAG 994 [137] | 23 (p) | 25,000 (p) | Inactive (p) | nd |
| 14 | NNC 21-0136 [93] | 10 (r) | 630 (r) | nd | nd |
| A2A-selective agonists | |||||
| 15 | CGS21680 | 289 (h) [109] | 27 (h) [109] | >10,000 (h) [109] | 67 (h) [109] |
| 1800 (r) [134] | 19 (r) [134] | ||||
| 120 (rb) [134] | 584 (r) [134] | ||||
| >10,000 (r) [134] | 673 (rb) [134] | ||||
| 16 | Apadenoson (ATL-146e) [109] | 77 (h) | 0.5 (h) | nd | 45 (h) |
| 17 | ATL-313 | nd | nd | nd | nd |
| 18 | UK-432097 [44] | nd | 4 (h) | nd | nd |
| 19 | Regadenoson (CV-3146) [109] | >10,000 (h) | 290 (h) | >10,000 (h) | > 10,000 (h) |
| 20 | [138] | >10,000 (h) | 5.4 (h) | 9866 (h) | 1640 (h) |
| 21 | GW328267X [138] | 882 (h) | 2.3 (h) | 51 (h) | 4.2 (h) (antagonist) |
| 22 | Sonedenoson (MRE-0094) [139] | >10,000 (h) | 490 (h) | >10,000 (h) | nd |
| 23 | Binodenoson (WRC-0470) [45] | 48,000 (h) | 270 (h) | 430,000 (h) | 903 (h) |
| 25 | [45] | 400 (r) | 372 (r) | nd | 3640 (h) |
| 50 (m) | |||||
| A2B-selective agonists | |||||
| 26 | [46] | 1050 (h) | 1550 (h) | 82 (h) | > 5000 (h) |
| 27 | MRS3997 [47] | 253 (h) | 150 (h) | 128 (h) | 90 (h) |
| 28 | BAY 60-6583 | >10,000 (h)c, [140] | > 10,000 (h)c, [140] | 3–10 (h) [140] | > 10,000 (h)c, [140] |
| 330 (m)e, [141] | |||||
| 750 (d)e, [141] | |||||
| 340 (rb)e, [141] | |||||
| A3-selective agonist | |||||
| 29 | IB-MECA (CF101) [109] | 51 (h) | 2900 (h) | 11,000 (h) | 1.8 (h) |
| 30 | Cl-IB-MECA (CF102) | 220 (h) [109] | 5360 (h) [109] | >10,000 (h) [134] | 1.4 (h) [109] |
| 280 (r) [134] | 470 (r) [134] | 0.33 (r) [134] | |||
| 35 (m) [134] | ~10,000 (m) [134] | >10,000 (m) [134] | 0.18 (m) [134] | ||
| 31 | [51] | 245 (h) | > 10,000 (h) | nd | 2.25 (h) |
| 32 | [52] | 32,800 (h) | 41,700 (h) | >30,000 (h) | 0.44 (h) |
| 33 | LJ529 [142] | 193 (h) | 223 (h) | nd | 0.38 (h) |
| 34 | MRS3558 (CF502) | 260 (h) [109] | 2330 (h) [109] | >10,000 (h) [109] | 0.29 (h) [109] |
| 105 (r) [134] | 1080 (r) [134] | 1.0 (r) [134] | |||
| 15.8 (m) [134] | 10,400 (m) [134] | 1.49 (m) [134] | |||
| 35 | MRS5151 [143] | 14,900 (h) | ~10,000 (h) | nd | 2.38 (h) |
| 10,500 (m) | > 10,000 (m) | 24.4 (m) | |||
| 36 | CP608,039 [144] | 7300 (h) | nd | nd | 5.8 (h) |
| 1750 (rb) | 83 (rb) | ||||
| 37 | CP532,903 [103] | 898 (m) | > 10,000 (m) | >10,000 (m) | 9.0 (m) |
a
h = human; d = dog; m = mouse; p = pig; r = rat; rb = rabbit.
b
Most data are from functional studies.
c
Data from functional studies.
d
nd = no data available.
e
Data from radioligand binding studies versus the antagonist radioligand [3H]MRS1754.