Table 2.
A1 Adenosine receptor affinity | |||
---|---|---|---|
Human | Rat | Mouse | |
Agonists | K i ± SEM (nM) vs. [3H]CCPAa | ||
NECA | 14 [49] | 5.1 [54] | 2.49 ± 0.15 |
CADO | 1.39 [3] | 6.7 [54] | 2.79 ± 0.04 |
CCPA | 0.83 [49] | 7.43 [55] | 0.269 ± 0.064 |
R-PIA | 2.04 [49] | 1.2 [56] | 0.587 ± 0.070 |
CGS-21680 | 289 [49] | 1800 [56] | 961 ± 108 |
BAY60-6583 | 387 ± 70 | 514 ± 57 | 351 ± 19 |
IB-MECA | 51 [57] | 54 [58] | 16.4 ± 1.7 |
CI-IB-MECA | 220 [57] 115 [3] |
820 [59] | 46.2 ± 3.6 |
Antagonists | K i ± SEM (nM) vs. [3H]DPCPXa | ||
Caffeine | 44,900 [60] 10,700 [61] |
18,800 [46] 41,000 [62] |
50,700 ± 5800 |
Theophylline | 6200 [46] | 8500 [46] | 14,200 ± 6000 |
CGS-15943 | 3.5 [56] | 6.4 [56] | 1.15 ± 0.16 |
DPCPX | 3.0 [63] | 0.50 [64] | 0.413 ± 0.064 |
PSB-36 | 0.7 [5] | 0.124 [60] | 1.58 ± 0.18 |
PSB-63 | 90.6 [5] | 16.9 [5] | 2370 ± 475 |
CPT | 23.7 ± 2.4 | 24 [5] 6.3 [65] |
7.41 ± 0.41 |
Istradefylline | 841 [5] | 230 [46] 150 [66] |
438 ± 93 |
ZM-241385 | 774 [56] | 684 ± 63 | 236 ± 36 |
Preladenant | >1000 [56] | >1000 | 462 ± 118 |
PSB-601 | 2070 [44] | 260 [44] | 123 ± 25 |
PSB-603 | >10,000 [46] | >10,000 [46] | 42.4 ± 4.2 |
PSB-1115 | >10,000 [46] | 2200 [45] | 591 ± 63 |
PSB-0788 | 2240 [46] | 386 [46] | 118 ± 21 |
MRS-1754 | 403 [67] | 16.8 [67] | 1.45 ± 0.42 |
MRS-1523 | >10,000 [56] | 15,600 [68] | >10,000 |
aData are means ± SEM of three independent assays performed in duplicates. The values without SEM are taken from the literature as indicated