JNJ-42253432 is a potent, selective, CNS-penetrant P2X7 antagonist with pKi of 9.1 and 7.9 for rat and huamn P2X7 channel, respectively.
JNJ-42253432 does not block calcium flux via human P2X1, P2X2, P2X3, P2X2/P2X3, and P2X4 at 10 uM.
JNJ-42253432 attenuates both ATP- and Bz-ATP-induced currents from hP2X7-1321N1 cells with similar potencies (pEC50=7.0).
JNJ-42253432 blocks the release of IL-1β induced by Bz-ATP in freely moving rat brain, also increases serotonin levels.
JNJ-42253432 attenuates amphetamine-induced hyperactivity in vivo.
