JNJ-42253432 |
| Catalog No.GC64822 |
JNJ-42253432는 CNS 침투성, 고친화성 및 경구 활성 P2X7 길항제이며 쥐 및 인간 P2X7 채널에 대해 각각 pKi 값이 9.1 및 7.9입니다.
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Cas No.: 1428327-35-8
Sample solution is provided at 25 µL, 10mM.
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JNJ-42253432 is a CNS-penetrant, high-affinity and orally active P2X7 antagonist, with pKi values of 9.1 and 7.9 for rat and human P2X7 channels, respectively[1].
When dosed in rats, JNJ-42253432 occupied the brain P2X7 channel with an ED50 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 ED50 of 10 mg/kg for SERT occupancy[1].
[1]. Brian Lord, et al. Pharmacology of a novel central nervous system-penetrant P2X7 antagonist JNJ-42253432. J Pharmacol Exp Ther. 2014 Dec;351(3):628-41.
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