JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology.
IC50&Target
pKi: 7.9 (huaman P2X7), 8.7 (rat P2X7)
体外研究
JNJ-47965567 exhibits high affinity for human and rat P2X7 in membrane preparations of 1321N1 cells.
JNJ-47965567 does not block IL-6 and TNF-α release, under identical conditions (LPS and BZ-ATP) used for IL-1β and IL-18 release.
JNJ-47965567 attenuates IL-1β release with pIC50s of 6.7 ± 0.07 (human blood), 7.5 ± 0.07 (human monocytes) and 7.1 ± 0.1 (rat microglia), respectively, in native systems.
体内研究
JNJ-47965567 (30-100 mg/kg; s.c.) attenuates IL-1β release induced by Bz-ATP.
JNJ-47965567 (30 mg/kg) attenuates amphetamine-induced hyperactivity and exhibits modest, yet significant efficacy in the rat model of neuropathic pain.
Animal Model:
Male Sprague Dawley rats
Dosage:
30 mg/kg, 100 mg/kg
Administration:
Subcutaneous injection; 30 minutes prior to Bz-ATP infusion
Result:
Significantly attenuated IL-1β release at 100 mg/kg, with no effect at 30 mg/kg dose group.
分子式
C28H32N4O2S
分子量
488.64
CAS号
1428327-31-4
运输条件
Room temperature in continental US; may vary elsewhere.