NSP-805

NSP-805 is a potent and selective inhibitor of guinea pig cardiac phosphodiesterase 3 (PDE3) , and a cardiotonic agent with vasodilator properties. In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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