JNJ-42253432 |
| Catalog No.GC64822 |
JNJ-42253432 est un antagoniste P2X7 pénétrant dans le SNC, de haute affinité et actif par voie orale, avec des valeurs de pKi de 9,1 et 7,9 pour les canaux P2X7 du rat et de l'homme, respectivement .
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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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