Product IntroductionBioactivity英文名:
PF-04859989 HCl描述: PF-04859989 HCl 是不可逆的犬尿氨酸转氨酶 KAT II 抑制剂,可透过血脑屏障,抑制 hKATⅡ 和 rKATⅡ 的 IC50分别为 23 和 263 nM。它对 KATⅡ 的选择性高于人 KATⅠ、KATⅢ 和 KATⅣ (IC50分别为22、11和 >50 μM)。
体外活性: The IC50s values are 23 and 263 nM for hKAT II and rKAT II. PF-04859989 HCl is selective for KAT II over human KAT I, KAT III, and KAT IV (IC50s of 22, 11, and >50 μM, respectively)[3].
体内活性: Acute administration of the KAT II inhibitor PF-04859989 (5 or 10 mg/kg) was associated with a short-onset, time-dependent decrease in firing rate and burst activity of DA neurons, both parameters reaching a 50% reduction within 45 min. Furthermore, PF-04859989 reduced the number of spontaneously active DA cells as measured 4-6 after administration. Pretreatment with d-cycloserine (30 mg/kg) or CGP-52432 (10 mg/kg) prevented the inhibitory action of PF-04859989 (5 mg/kg) on firing rate and burst firing activity. In contrast, pretreatment with methyllycaconitine (MLA, 4 mg/kg) did not change the response, whereas picrotoxin (4.5 mg/kg) partially prevented the inhibitory effects of PF-04859989 (5 mg/kg, i.v.)[2].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 100 mg/mL (465.87 mM)
H2O : 100 mg/mL (465.87 mM)
关键字:
disorders |
schizophrenia |
Inhibitor |
inhibit |
PF04859989 HCl |
midbrain |
psychiatric |
PF 04859989 HCl |
dopamine |
neurons |
PF-04859989 HCl |
cognitive ,impairment相关库:
Bioactive Compounds Library Max |
Inhibitor Library |
Bioactive Compound Library