JNJ-47965567 is a potent, selective, centrally permeable P2X7 receptor antagonist with pKi of 7.9 and 8.7 for human and rat P2X7, respectively.
JNJ-47965567 attenuates IL-1β release with pEC50 of 6.7 (human blood), 7.5 (human monocytes) and 7.1 (rat microglia).
JNJ-47965567 exhibits target engagement in rat brain with brain EC50 of 78 ± 19 ng/ml, as well as functional block of Bz-ATP induced IL-1β release.
JNJ-47965567 attenuateas amphetamine-induced hyperactivity and exhibits modest, yet significant efficacy in the rat model of neuropathic pain.
