JNJ-47965567

JNJ-47965567 is a potent and selective antagonist of the purinergic receptor P2X subtype 7 (P2X7), a ligand-gated ion channel. Activation of P2X receptors by BzATP induces calcium flux. JNJ-47965567 attenuates Bz-ATP induced calcium flux in 1321N1 astrocytoma cells transfected with the recombinant P2X7 proteins with pIC₅₀ values of 8.3, 7.5 and 7.2 for human, mouse and rat receptors respectively. JNJ-47965567 (30 mg/kg for 5 days) significantly reduces spontaneous seizures in epileptic mice even after treatment is stopped.