Table 2.
Summary of rhesus macaque and human P2X7 receptor pharmacology
| rmP2X7 | hP2X7 | |
|---|---|---|
| ATP | (n = 11) | (n = 12) |
| EC50 (mM) | 0.8 ± 0.09***††† | 0.3 ± 0.02*** |
| Hill coefficient | 1.2 ± 0.06***††† | 1.9 ± 0.06 |
| BzATP | (n = 6) | (n = 5) |
| EC50 (µM) | 58 ± 4††† | 30 ± 2 |
| Hill coefficient | 1.9 ± 0.1 | 2.2 ± 0.2 |
| KN-62 | (n = 3) | (n = 3) |
| IC50 (nM) | 86 ± 19 (54 ± 8a) | 130 ± 40 |
| Hill coefficient | 1.2 ± 0.4 (1.9 ± 0.2a) | 1.6 ± 0.2 |
| AZ11645373 | (n = 3) | (n = 3) |
| IC50 (nM) | 23 ± 3 | 31 ± 3 |
| Hill coefficient | 1.2 ± 0.1 | 1.8 ± 0.5 |
| A-438079 | (n = 6) | (n = 6) |
| IC50 (nM) | 297 ± 24 | 493 ± 94 |
| Hill coefficient | 0.8 ± 0.05†† | 1.1 ± 0.1 |
***
P < 0.001, compared between ATP and BzATP within the same species;
††
P < 0.01
†††
P < 0.001 compared between rmP2X7 and hP2X7 receptors.
a
Results from fitting the data to the Hill equation with three parameters.