Antagonist | Human | Rat | Mouse |
---|---|---|---|
PPADS | 7.9 ± 0.1 | 6.9 ± 0.11-150 | 5.2 ± 0.11-150 1-159 |
P5P | 6.9 ± 0.1 | 6.4 ± 0.2 | 5.1 ± 0.21-150 1-159 |
KN62 | 7.7 ± 0.1 | <51-150 | 6.7 ± 0.21-150 1-159 |
OxATP | 5.5 ± 0.1 | 4.6 ± 0.11-150 | 4.2 ± 0.11-150 |
Studies were conducted in sucrose buffer at 37°C using suspensions of cells expressing human, rat, or mouse P2X7 receptors. Antagonists were preincubated with cells for 30 min before addition of BzATP and YO-PRO-1. Incubations were allowed to proceed until approximately 20 to 80% of the maximal response had occurred before measuring cell-associated fluorescence. Data represent pIC50values determined against an approximate EC50 concentration of BzATP and are the mean ± S.E.M. of four to six experiments.