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125068-54-4

中文名稱 125068-54-4
英文名稱 NSP 805
CAS 125068-54-4
分子式 C17H19N3O2
分子量 297.35
MOL 文件 125068-54-4.mol
125068-54-4 結(jié)構(gòu)式 125068-54-4 結(jié)構(gòu)式

基本信息

中文別名
化合物NSP-805
英文別名
NSP 805
3(2H)-Pyridazinone, 4,5-dihydro-5-methyl-6-[4-[(2-methyl-3-oxo-1-cyclopenten-1-yl)amino]phenyl]-

物理化學(xué)性質(zhì)

密度1.30±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)13.84±0.60(Predicted)
形態(tài)Solid
顏色Light yellow to yellow

常見(jiàn)問(wèn)題列表

生物活性
NSP-805 是一種有效的,選擇性的 phosphodiesterase 3 (PDE3) 抑制劑,為一種強(qiáng)心劑,具有舒張血管的作用。
體外研究

In isolated guinea pig left atria, NSP-805 shows positive inotropic EC 50 value in order of potency of 0.18 μM. The in vitro positive inotropic effects of NSP-805 is accompanied by increases in tissue cyclic AMP and abolished by carbachol.

體內(nèi)研究

In anesthetized dogs, intravenous (i.v.) injection of NSP-805 produces dose-dependent increases in left ventricular VVdp/dtmax and decreases in aortic blood pressure (ABP) with relatively small increases in heart rate (HR). The ED 50 value for LVdP/dtmax of NSP-805 is 12 μg/kg. When the drugs is administered intraduodenally to anesthetized dogs, the ED 50 value for LVdP/dtmax of NSP-805, is approximately 10 μg/kg. In the propranolol-induced heart failure model, NSP-805 completely improves the hemodynamic state of heart failure to normal levels. NSP-805(100 μg/kg) reduces systemic blood pressure significantly, but the increase of chorio-retinal blood flow is less than that at the low dose of NSP-805 (40 μg/kg) in rabbit eyes.

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