Anindya Bhattacharya, Qi Wang, Hong Ao, James R Shoblock, Brian Lord, Leah Aluisio, Ian Fraser, Diane Nepomuceno, Robert A Neff, Natalie Welty, Timothy W Lovenberg, Pascal Bonaventure, Alan D Wickenden, Michael A Letavic
BACKGROUND AND PURPOSE: An increasing body of evidence suggests that the purinergic receptor P2X, ligand-gated ion channel, 7 (P2X7) in the CNS may play a key role in neuropsychiatry, neurodegeneration and chronic pain. In this study, we characterized JNJ-47965567, a centrally permeable, high-affinity, selective P2X7 antagonist. EXPERIMENTAL APPROACH: We have used a combination of in vitro assays (calcium flux, radioligand binding, electrophysiology, IL-1β release) in both recombinant and native systems...
October 2013: British Journal of Pharmacology