125068-54-4

125068-54-4 structure

Name: NSP-805
Chemical Name: 4-methyl-3-[4-[(2-methyl-3-oxocyclopenten-1-yl)amino]phenyl]-4,5-dihydro-1H-pyridazin-6-one
CAS Number: 125068-54-4
Molecular Formula: C₁₇H₁₉N₃O₂
Molecular Weight: 297.35200
Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphodiesterase (PDE)
Create Date: 2017-12-01 01:00:29
Modify Date: 2024-01-11 13:50:28
NSP-805 is a potent and selective inhibitor of guinea pig cardiac phosphodiesterase 3 (PDE3), and a cardiotonic agent with vasodilator properties.

Name	4-methyl-3-[4-[(2-methyl-3-oxocyclopenten-1-yl)amino]phenyl]-4,5-dihydro-1H-pyridazin-6-one
Synonyms	Nsp 805 3(2H)-Pyridazinone,4,5-dihydro-5-methyl-6-[4-[(2-methyl-3-oxo-1-cyclopenten-1-yl)amino]phenyl] NSP-805

Description	NSP-805 is a potent and selective inhibitor of guinea pig cardiac phosphodiesterase 3 (PDE3), and a cardiotonic agent with vasodilator properties.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE) Research Areas >> Cardiovascular Disease
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[1].
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[1]. 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[2].
References	[1]. Mochizuki N, et al. Cardiovascular effects of NSP-804 and NSP-805, novel cardiotonic agents with vasodilator properties. J Cardiovasc Pharmacol. 1993 Jun;21(6):983-95. [2]. Uchida H, et al. [The effect of phosphodiesterase type 3 inhibitor on chorio-retinal blood flow in rabbits eyes]. Nippon Ganka Gakkai Zasshi. 2002 Oct;106(10):615-20.

Density	1.3g/cm3
Molecular Formula	C₁₇H₁₉N₃O₂
Molecular Weight	297.35200
Exact Mass	297.14800
PSA	74.05000
LogP	2.38000
Index of Refraction	1.656
Storage condition	2-8℃

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