Table 3.
No. | Compound | Affinity, pKia | |||
---|---|---|---|---|---|
A1 | A2A | A2Bb | A3 | ||
Adenosine receptor agonists | |||||
1 | adenosineb | ~7 7.14 (r) |
6.49 6.82 (r) |
4.82 5.29 (r) |
6.54 5.19 (r) |
A1-selective | |||||
2 | R-PIA | 8.69 8.92 (r) |
6.66 (r) | 3.82 | 7.48 6.80 (r) |
3 | CPA | 8.64 | 6.10 | 4.73 | 7.14 |
4 | CCPA | 9.08 8.89 (r) |
5.64 6.02 (r) |
4.73 | 7.42 6.63 (r) |
5 | 5′-Cl-5′-deoxy-ENBA | 9.29 | 5.89 | 5.87 | 5,56 |
A2A-selective | |||||
6 | CGS21680 | 6.54 5.74 (r) |
7.57 7.72 (r) |
<5 <5 (r) |
7.17 6.23 (r) |
7 | UK432,097 | ND | 8.4 | ND | ND |
A2B-selective | |||||
8 | BAY 60-6583 | <5b | <5b | 8–8.5 | <5b |
A3-selective | |||||
9 | IB-MECA (CF101) | 7.29 | 5.54 | 4.96 | 8.74 |
10 | Cl-IB-MECA (CF102) | 6.66 6.55 (r) |
5.27 6.33 (r) |
<5 | 8.85 9.48 (r) |
11 | thio-Cl-IB-MECA | 6.71 | 6.63 | ND | 9.42 |
12 | MRS5698 | <5 | <5 | <5 | 8.5 |
Adenosine receptor antagonists | |||||
Non-selective | |||||
13 | Caffeine | 4.97 4.39 (r) |
5.02 4.32 (r) |
4.98 4.52 (r) |
4.88 <4 (r) |
14 | Theophylline | 5.17 5.06 (r) |
5.17 25,300 (r) |
5.04 4.82 (r) |
4.65 4.07 (r) |
15 | CGS15943 | 8.46 8.19 (r) |
8.92 | 7.49 | 7.46 |
16 | XAC | 7.54 8.92 (r) |
9.0 7.20 (r) |
7.91 | 7.04 |
A1-selective | |||||
17 | DPCPX (CPX) | 8.52 9.0 (r) |
7.22 6.30 (r) |
7.29 6.73 (r) |
6.61 4.37 (r) |
18 | PSB-36 | 9.2 9.91 (r) |
6.01 6.26 (r) |
6.73 | 5.64 5.19 (r) |
A2A-selective | |||||
19 | KW6002 | 6.08b 6.64(r)b |
7.92 8.66 (r) |
<5b | 5.35b |
20 | CSCd | 4.55 (r) | 7.27 (r) | 5.09 | <5 (r) |
21 | ZM241,385 | 6.11 | 8.80 | 7.12 | 6.13 |
22 | SCH442,416 | 5.95 | 8.39 | <5 | <5 |
A2B-selective | |||||
23 | MRS1754 | 6.39 7.77 (r) |
6.30 6.21 (r) |
8.70 7.89 (r) |
6.24 |
24 | MRS1706 | 6.80 | 6.91 | 8.86 | 6.64 |
25 | MRE2029-F20 | 6.70 | <6 | 8.26 | <6 |
26 | PSB-603 | <5 <5 (r) |
<5 <5 (r) |
9.26 | <5 |
27 | PSB-1115 | <5 5.66 (r) |
4.62 (r) | 7.27 | <5 |
A3-selective | |||||
28 | MRS1523 | <5 4.81 (r) |
5.44 5.69 (r) |
<5 | 7.72 6.95 (r) |
29 | PSB-10 | 5.77 6.09 (r) |
5.57 5.22 (r) |
ND | 9.36 |
30 | VUF5574 | ≤5 (r) | ≤5 (r) | ND | 8.39 |
31 | MRS1191 | <5 4.40 (r) |
<5 <5 (r) |
<5 | 7.50 5.73 (r) |
32 | MRS1334 | <5 (r) | <5 (r) | ND | 8.57 |