Name | NSP 805 |
Synonyms | NSP 805 3(2H)-Pyridazinone, 4,5-dihydro-5-methyl-6-[4-[(2-methyl-3-oxo-1-cyclopenten-1-yl)amino]phenyl]- |
CAS | 125068-54-4 |
Molecular Formula | C17H19N3O2 |
Molar Mass | 297.35 |
Density | 1.30±0.1 g/cm3(Predicted) |
pKa | 13.84±0.60(Predicted) |
Storage Condition | Room Temprature |
In vitro study | 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. |
In vivo study | 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. |
biological activity | NSP-805 is a potent, selective phosphoristerase 3 (PDE3) inhibitor, it has the effect of relaxing blood vessels. |