A-740003 (A740003) is a potent, selective, competitive P2X7 receptor antagonist with IC50 of 40 nM and 18 nM for hP2X7 and rP2X7, respectively.
A-740003 showed weak or no activity for other P2 receptors (IC50>10 uM); potently blocks agonist-evoked IL-1β release (IC50=156 nM) and pore formation (IC50=92 nM) in differentiated human THP-1 cells.
A-740003 produces dose-dependent antinociception in a spinal nerve ligation model (ED50=19 mg/kg i.p.) in the rat.
