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]:
[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]
[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℃