Competition studies on the rat recombinant P2X4purinoceptor
| Compound | pIC50 | Hill slope |
|---|---|---|
| ATP | 9.32 ± 0.12 | 0.92 ± 0.03 |
| ATPγS | 9.17 ± 0.06 | 0.96 ± 0.04 |
| 2-Me-S-ATP | 8.66 ± 0.09 | 0.94 ± 0.05 |
| αβ-MeATP | 7.82 ± 0.11 | 0.99 ± 0.02 |
| ADP | 7.48 ± 0.05 | 1.01 ± 0.04 |
| βγ-MeATP | 7.11 ± 0.10 | 0.95 ± 0.06 |
| l-βγ-MeATP | 5.71 ± 0.16 | 0.84 ± 0.01 |
| αβMeADP | 4.66 ± 0.16 | 0.97 ± 0.03 |
| Dextran1-a | 0.88 ± 1.60 | 0.15 ± 0.04 |
| DIDS1-a | 1.10 ± 0.28 | 0.41 ± 0.03 |
| PPADS | 3.33 ± 0.18 | 0.26 ± 0.08 |
| P5P | 2.89 ± 0.10 | 1.35 ± 0.35 |
| Cibacron blue | 5.03 ± 0.17 | 0.46 ± 0.03 |
| Suramin | 3.27 ± 0.14 | 0.50 ± 0.02 |
| Coomassie blue | 3.93 ± 0.30 | 0.25 ± 0.00 |
Competition binding studies were performed in membranes prepared from CHO-K1 cells infected with the rat P2X4 purinoceptor using a Semliki Forest virus construct. The concentration of [35S]ATPγS was 0.1–0.2 nM. Data are mean ± standard error of three to five determinations.
↵1-a pIC50 value estimated is in excess of the highest concentration of the compound tested.