Biological Activity: | 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). |