JNJ-42253432

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

References 1. Lord B, et al. J Pharmacol Exp Ther. 2014 Dec;351(3):628-41. 2. Amhaoul H, et al. Neuropharmacology. 2016 Jun;105:175-185. View Related Products by Target P2X Receptor