A selective P2X7 receptor antagonist.
Potent and selective human P2X 7 antagonist (K B values are 5 - 7 and > 10,000 nM at hP2X 7 and rP2X 7 respectively) that is completely without effect at all other P2X subtypes. Inhibits BzATP-mediated calcium influx and inhibits ATP-mediated IL-1 β release in vitro (K B values are 15 and 92 nM respectively).
1. stokes l, jiang lh, alcaraz l, et al. characterization of a selective and potent antagonist of human p2x(7) receptors, az11645373. british journal of pharmacology. 2006;149(7):880-887.