TABLE 2

Affinities of selected, useful adenosine receptor antagonists

Ki (nM)a
A1A2AA2BA3
Nonselective Antagonists
3Caffeine44,900 (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)
4Theophylline6,770 (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
17DPCPX (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)
18PSB-360.7 (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)
19SLV3201.00 (h)
2.51 (r)
398 (h)3,981 (h)
501 (r)
200 (h)
A2AAR-Selective Antagonists
5Istradefylline (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)
20MSX-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)
21Preladenant (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)
22Imaradenant (AZD4635)160 (h)1.7 (h)64 (h)>10,000 (h)
A2BAR-Selective Antagonists
23MRS1754403 (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)
24PSB-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)
25PSB-07882,240 (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)
26PSB-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)
27GS 6201 (CVT-6883)1,940 (h)3,280 (h)22 (h)1,070 (h)
28BAY-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)
29ISAM-140>1,000 (h)>1,000 (h)3.49 (h)>1,000 (h)
A3AR-Selective Antagonists
30MRS1523>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)
31MRE3008-F201200 (h)141 (h)2100 (h)0.82 (h)
32PSB-101,700 (h)
805 (r)
2,700 (h)
6,040 (r)
30,000 (h)0.441 (h)
17,000 (r)
33VUF5574≥10,000 (r)≥10,000 (r)n.d.4.03 (h)
34MRS7591b>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.