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CAS No. : 125068-54-4
MCE 国际站:NSP-805
产品活性:NSP-805 是一种有效的,选择性的 phosphodiesterase 3 (PDE3) 抑制剂,为一种强心剂,具有舒张血管的作用。
研究领域:Metabolic Enzyme/Protease
作用靶点:Phosphodiesterase (PDE)
In Vitro: In isolated guinea pig left atria, NSP-805 shows positive inotropic EC50 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.
In Vivo: 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 ED50 value for LVdP/dtmax of NSP-805 is 12 μg/kg. When the drugs is administered intraduodenally to anesthetized dogs, the ED50 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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