产品
编 号:F213095
分子式:C9H11ClN2O2
分子量:214.65
产品类型
结构图
CAS No: 177943-33-8
联系客服
产品详情
生物活性:
PF-04859989 hydrochloride is a brain-penetrant, irreversible kynurenine aminotransferase (KAT) II inhibitor with IC50s of 23 and 263 nM for hKAT II and rKAT II. PF-04859989 hydrochloride is selective for KAT II over human KAT I, KAT III, and KAT IV (IC50s of 22, 11, and >50 μM, respectively).
体内研究:
In vivo pharmacokinetic and efficacy studies in rat show that PF-04859989 is a brain-penetrant, irreversible inhibitor and is capable of reducing brain kynurenic acid by 50% at a dose of 10 mg/kg (sc). Rats receiving PF-04859989 (5 mg/kg; i.p.) exhibited a significantly lower number of spontaneously active DA neurons pertrack.Animal Model:Male Sprague-Dawley rats
Dosage:5 mg/kg
Administration:I.p.
Result:Exhibited a significantly lower number of spontaneously active dopamine (DA) neurons pertrack compared to controls.