Table 2.
Adenosine receptor in vitro potency
| Compound | A2a human CHO-K1 cells | rTNFα splenocytes | ||||
|---|---|---|---|---|---|---|
| EC50 (nmol/L) | Intrinsic activity (%) | n | IC50 (nmol/L) | Intrinsic activity (%) | n | |
| CGS21680 | 62.8 (16.8) | 94.3 (7.8) | 2 | 6.9 (2.8) | 63.5 (8) | 8 |
| UK-432,097 | 5.4 (1.8) | 94.8 (5.5) | 3 | 2.6 (1.2) | 60.9 (2.6) | 2 |
| 1 | 2.4 (0.3) | 102 (6.7) | 7 | 3.2 (2.5) | 53.4 (4.3) | 4 |
| 2 | 1.4 (0.5) | 97.9 (4.9) | 7 | 0.6 (0.1) | 57.4 (5.4) | 6 |
| 3 | 0.4 (0.2) | 96.2 (12.9) | 3 | 0.2 (0.1) | 58 (10.5) | 4 |
EC50 and intrinsic activity values correspond to averages, standard deviations are in brackets. EC50, half maximal effective concentration; IC50, half maximal inhibitory concentration.