NSP-805

Names

[ CAS No. ]:
125068-54-4

[ Name ]:
NSP-805

[Synonym ]:
Nsp 805
3(2H)-Pyridazinone,4,5-dihydro-5-methyl-6-[4-[(2-methyl-3-oxo-1-cyclopenten-1-yl)amino]phenyl]
NSP-805

Biological Activity

[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.


[Related Small Molecules]

3-Isobutyl-1-methylxanthine | rolipram | PF-04957325 | AN-2728 | GLPG1690 | BAY-60-7550 | Icariin | Ibudilast | PF-8380 | TAK-063 | Dipyridamole | Cilostazol | GSK256066 | Cialis | Pentoxifylline

Chemical & Physical Properties

[ 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℃


Related Compounds