177943-33-8
中文名稱(chēng)
(S)-3-aMino-1-hydroxy-3,4-dihydroquinolin-2(1H)-one hydrochloride
CAS
177943-33-8
分子式
C9H11ClN2O2
分子量
214.649
MOL 文件
177943-33-8.mol
177943-33-8 結(jié)構(gòu)式
基本信息
英文別名
177943-33-8PF04859989 hydrochloride
PF-4859989 hydrochloride
PF-04859989 hydrochloride
PF-04859989 hydrochloride >=98% (HPLC)
(3S)-3-Amino-1-hydroxy-3,4-dihydroquinolin-2(1H)-one
L-3-Amino-3,4-dihydro-1-hydroxycarbstyril hydrochloride
(S)-3-aMino-1-hydroxy-3,4-dihydroquinolin-2(1H)-one hydrochloride
2(1H)-Quinolinone, 3-amino-3,4-dihydro-1-hydroxy-, monohydrochloride, (S)- (9CI)
PF 04859989 hydrochloride - L-3-Amino-3,4-dihydro-1-hydroxycarbstyril hydrochloride
常見(jiàn)問(wèn)題列表
生物活性
PF-04859989 hydrochloride 是一種可透過(guò)血腦屏障的，不可逆的犬尿氨酸轉(zhuǎn)氨酶 KAT II 抑制劑，對(duì) hKATⅡ 和 rKATⅡ 的 IC50 分別為 23 和 263 nM。PF-04859989 hydrochloride 對(duì) KATⅡ 的選擇性高于人 KATⅠ、KATⅢ 和 KATⅣ (IC50 分別為22、11和 >50 μM)。體內(nèi)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. |