TABLE 2.
Affinities of selected, useful adenosine receptor antagonists
| Ki (nM)a | |||||
|---|---|---|---|---|---|
| A1 | A2A | A2B | A3 | ||
| Nonselective Antagonists | |||||
| 3 | Caffeine | 44,900 (h) 41,000 (r) 50,700 (m) |
23,400 (h) 43,000 (r) 11,100 (m) |
33,800 (h) 30,000 (r) 23,000 (m) |
13,300 (h) >100,000 (r) >100,000 (m) |
| 4 | Theophylline | 6,770 (h) 14,000 (r) |
6,700 (h) 22,000 (r) |
9,070 (h) 15,100 (r) 5,630 (m) |
22,300 (h) >100,000 (r) |
| A1AR-Selective Antagonists | |||||
| 17 | DPCPX (CPX) | 3.0 (h) 0.50 (r) 0.413 (m) |
129 (h) 157 (r) 263 (m) |
51 (h) 186 (r) 86.2 (m) |
243 (h) >10,000 (r) >10,000 (m) |
| 18 | PSB-36 | 0.7 (h) 0.124 (r) 1.58 (m) |
980 (h) 552 (r) 697 (m) |
187 (h) 350 (r) 704 (m) |
2,300 (h) 6,500 (r) >10,000 (m) |
| 19 | SLV320 | 1.00 (h) 2.51 (r) |
398 (h) | 3,981 (h) 501 (r) |
200 (h) |
| A2AAR-Selective Antagonists | |||||
| 5 | Istradefylline (KW6002) | 841 (h) 230 (r) 438 (m) |
12 (h) 4.46 (r) 6.83 (m) |
>10,000 (h) 5,940 (r) 3,590 (m) |
4,470 (h) >10,000 (r) >10,000 (m) |
| 20 | MSX-3 / MSX-2 (Data are for MSX-2) |
2,500 (h) 900 (r) |
5.38 (h) 8.04 (r) |
>10,000 (h) | >10,000 (h) |
| 21 | Preladenant (SCH-420814) | >1,000 (h) >1,000 (h) 462 (m) |
0.9 (h) 0.986 (r) 0.241 (m) |
>1,000 (h) >1,000 (m) >1,000 (r) |
>1,000 (h) >1,000 (m) >1,000 (r) |
| 22 | Imaradenant (AZD4635) | 160 (h) | 1.7 (h) | 64 (h) | >10,000 (h) |
| A2BAR-Selective Antagonists | |||||
| 23 | MRS1754 | 403 (h) 16.8 (r) 1.45 (m) |
503 (h) 612 (r) >10,000 (m) |
1.97 (h) 12.8 (r) 3.12 (m) |
570 (h) >1,000 (m) >1,000 (r) |
| 24 | PSB-603 | >10,000 (h) >10,000 (r) 42.4 (m) |
>10,000 (h) >10,000 (r) >10,000 (m) |
0.553 (h) 0.355 (r) 0.265 (m) |
>10,000 (h) >10,000 (r) >10,000 (m) |
| 25 | PSB-0788 | 2,240 (h) 386 (r) 118 (m) |
333 (h) 1,730 (r) 235 (m) |
0.393 (h) 2.12 (r) 1.90 (m) |
>1,000 (h) >10,000 (r) >10,000 (m) |
| 26 | PSB-1115 | >10,000 (h) 2,200 (r) 591 (m) |
3790 (h) 24,000 (r) >10,000 (m) |
53.4 (h) 3,140 (r) 1,940 (m) |
>10,000 (h) >10,000 (r) >10,000 (m) |
| 27 | GS 6201 (CVT-6883) | 1,940 (h) | 3,280 (h) | 22 (h) | 1,070 (h) |
| 28 | BAY-545 | >1,000; 1,300 (h) n.d. (r) >6,700 (m) |
>1,000; 820 (h) 750 (r) 470 (m) |
59–97 (h) 280 (r) 400 (m) |
>10,000 (h) n.d. (r) >6,700 (m) |
| 29 | ISAM-140 | >1,000 (h) | >1,000 (h) | 3.49 (h) | >1,000 (h) |
| A3AR-Selective Antagonists | |||||
| 30 | MRS1523 | >10,000 (h) 15,600 (r) >10,000 (m) |
3660 (h) 2050 (r) >10,000 (m) |
>10,000 (h) >10,000 (r) >10,000 (m) |
18.9 (h) 113 (r) 731 (m) |
| 31 | MRE3008-F20 | 1200 (h) | 141 (h) | 2100 (h) | 0.82 (h) |
| 32 | PSB-10 | 1,700 (h) 805 (r) |
2,700 (h) 6,040 (r) |
30,000 (h) | 0.441 (h) 17,000 (r) |
| 33 | VUF5574 | ≥10,000 (r) | ≥10,000 (r) | n.d. | 4.03 (h) |
| 34 | MRS7591b | >10,000 (h) 590 (m) |
>10,000 (h) n.d. |
n.d. n.d. |
10.9 (h) 17.8 (m) |
h, human; Ki, inhibition constant; m, mouse; n.d., no data; r, rat.
adata are taken from the literature cited in the text.
bpartial agonistic activity if receptor is highly expressed.