JNJ-55308942

JNJ-55308942 is a novel highly potent P2X7 antagonist with Ki of 1.0 and 6.5 nM for rat and human hP2X7, demonstrates significant activity against a panel of related P2X receptors (P2X1, P2X2, P2X3, P2X2/3, and P2X4; also shows insignificant inhibition of nine CYP isoforms (IC50>15 uM); exhibits excellent P2X7 receptor occupancy in the hippocampus of rats with low ED50 of 0.07 mg/kg and unbound plasma EC50 of 12 ng/mL, suppresses brain IL-1β release in vivo in freely moving rats challenged with the P2X7 agonist Bz-ATP; possesses good tolerability margins in preclinical species, as well as an acceptable cardiovascular safety profile in vivo. Epilepsy Phase 1 Clinical

References 1. Chrovian CC, et al. J Med Chem. 2018 Jan 11;61(1):207-223. View Related Products by Target P2X Receptor Epilepsy