Potent and selective P2X7 antagonist (IC50 values 10 nM, 9 nM, and 11 nM for rat, mouse, and human receptors respectively). A 804598 potently blocked agonist stimulated release of IL-1β and Yo-Pro uptake from differentiated THP-1 cells that natively express human P2X7 receptors.In another study, A 804598 was found to produce a concentration-dependent inhibition of BZ-ATP-stimulated calcium influx (IC50 value 28.71 nM) in cells expressing the rat recombinant P2X7 receptor; a useful tool for autoradiographic localization of P2X7 receptors in the rat brain and spinal cord.