Table 2.
Effects of selective P2X 7 antagonists at GOF and LOF P2X 7 variants
|
Yo-Pro-1 uptake (IC
50
, nM) |
Ca
2+
flux (IC
50
, nM) |
|||||||
|---|---|---|---|---|---|---|---|---|
| WT | 155Tyr | 348Thr | 496Ala | WT | 155Tyr | 348Thr | 496Ala | |
|
A-804598 |
21.77 ± 2.8 |
21.50 ± 5.8 |
15.5 ± 0.6 |
ND |
20.81 ± 7.6 |
19.36 ± 6.9 |
40.7 ± 14.2 |
25.57 ± 1.6 |
|
A740003 |
332.83 ± 12.3 |
449.2 ± 12.7 |
415.9 ± 98.2 |
ND |
507.87 ± 91.1 |
379.43 ± 135.1 |
720.75 ± 27.9 |
405.50 ± 81.7 |
| AZ11645373 | 198.2 ± 42 | 342.6 ± 48.3 | 218.75 ± 113.5 | ND | 296.3 ± 98.5 | 510 ± 39.9 | 806.75 ± 249.3 | 412.40 ± 1.7 |
IC50 values reported here represent the averages ± SEM of 3 separate experiments. For simplicity Hill slope were not included in the table. Data for Yo-Pro-1 uptake assay for 496Ala variant could not be determined (ND) due to the low amplitude of responses obtained with this variant.