TABLE 1.
Antagonist sensitivity at chimeric P2X7Rs
RESIZEMean pIC50 values ± S.E.M. and fold change in sensitivity relative to P2X7-2Nβ are shown for the antagonists A740003 and A438079 at chimeric P2X7Rs. n numbers are shown for each receptor tested.
| A740003 |
A438079 |
|||
|---|---|---|---|---|
| pIC50 ± S.E.M. | n | pIC50 ± S.E.M. | n | |
| P2X7-2Nβ | 7.1 ± 0.05 | 6 | 6.0 ± 0.05 | 4 |
| 73–79 | 7.1 ± 0.04 | 3 | 6.7 ± 0.05** | 6 |
| 81–88 | 7.1 ± 0.13 | 3 | 6.0 ± 0.06 | 3 |
| 89–94 | 6.6 ± 0.06** | 3 | <4**** | 3 |
| 105–114 | 7.0 ± 0.04 | 3 | 6.3 ± 0.08 | 4 |
| 112–118 | 6.6 ± 0.02** | 5 | 5.5 ± 0.01 | 3 |
| 122–128 | 7.0 ± 0.14 | 3 | 6.1 ± 0.18 | 4 |
| 164–168 | 6.4 ± 0.07**** | 4 | 5.0 ± 0.09**** | 3 |
| 170–177 | 7.2 ± 0.08 | 3 | 6.2 ± 0.03 | 3 |
| 210–217 | 7.1 ± 0.05 | 3 | 6.6 ± 0.06* | 4 |
| 279–285 | 6.2 ± 0.10**** | 3 | 4.5 ± 0.05**** | 4 |
| 280–284 of P2X4 | 6.1 ± 0.05**** | 3 | 4.5 ± 0.05**** | 3 |
| 295–310 | 6.3 ± 0.07**** | 3 | 5.0 ± 0.06**** | 3 |
*
P < 0.05;
**
P < 0.01;
****
P < 0.0001.