compound introduction
JNJ-42253432 is a CNS-penetrant, high-affinity and orally active P2X7 antagonist, with pK i values of 9.1 and 7.9 for rat and human P2X7 channels, respectively. In Vivo When dosed in rats, JNJ-42253432 occupied the brain P2X7 channel with an ED 50 of 0.3 mg/kg, corresponding to a mean plasma concentration of 42 ng/ml. JNJ-42253432 also increased serotonin levels in the rat brain, which is due to antagonism of the serotonin transporter (SERT) resulting in an ED 50 of 10 mg/kg for SERT occupancy . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid
