N-((4-(4-フェニルピペラジン-1-イル)テトラヒドロ-2H-ピラン-4-イル)メチル)-2-(フェニルチオ)ニコチンアミド 化學(xué)特性,用途語(yǔ),生産方法
説明
JNJ-47965567 is a selective antagonist of the purinergic receptor P2X subtype 7 (P2X
7), a ligand-gated ion channel. Activation of P2X receptors by BzATP induces calcium flux, which is reduced by JNJ-47965567 in 1321N1 cells transfected with recombinant P2X
7 human, macaque, dog, rat, or mouse protein with pIC
50s of 8.3, 8.6, 8.5, 7.2, or 7.5, respectively. JNJ-47965567 suppresses neonatal hypoxia-induced seizures in mice and has some anticonvulsant properties in rats. It also reduces spontaneous seizures in epileptic mice even after treatment is stopped.
使用
2-(Phenylthio)-N-[[tetrahydro-4-(4-phenyl-1-piperazinyl)-2H-pyran-4-yl]methyl]-3-pyridinecarboxamide is a potent and selective human P2X7 antagonist.
Biochem/physiol Actions
JNJ-47965567 is a potent P2X7 antagonist with high affinity for the rat receptor (pKi = 8.7). It is centrally available after systemic injection with a superior brain:plasma distribution compared to other available P2X7 antagonists. JNJ-47965567 was shown to suppress epileptic seizures in a mouse model of epilepsy. It appears to have a disease modifying effect since spontaneous seizure rates did not increase once treatment with JNJ-477965567 was stopped.
N-((4-(4-フェニルピペラジン-1-イル)テトラヒドロ-2H-ピラン-4-イル)メチル)-2-(フェニルチオ)ニコチンアミド 上流と下流の製品情報(bào)
原材料
準(zhǔn)備製品