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NSP-805 Sale

目录号 : GC32572

NSP-805是一种有效的,选择性的phosphodiesterase3(PDE3)抑制剂,为一种强心剂,具有舒张血管的作用。

NSP-805 Chemical Structure

Cas No.:125068-54-4

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产品描述

NSP-805 is a potent and selective inhibitor of guinea pig cardiac phosphodiesterase 3 (PDE3), and a cardiotonic agent with vasodilator properties.

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 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].

[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.

Chemical Properties

Cas No. 125068-54-4 SDF
Canonical SMILES O=C1CC(C)C(C2=CC=C(NC3=C(C)C(CC3)=O)C=C2)=NN1
分子式 C17H19N3O2 分子量 297.35
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 3.363 mL 16.8152 mL 33.6304 mL
5 mM 0.6726 mL 3.363 mL 6.7261 mL
10 mM 0.3363 mL 1.6815 mL 3.363 mL
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Research Update

Cardiovascular effects of NSP-804 and NSP-805, novel cardiotonic agents with vasodilator properties

J Cardiovasc Pharmacol 1993 Jun;21(6):983-95.PMID:7687727DOI:10.1097/00005344-199306000-00021.

The cardiovascular properties of NSP-804 (4,5-dihydro-6-[4-[(2-methyl-3-oxo-1-cyclopentenyl)-amino] phenyl]-3(2H)-pyridazinone) and NSP-805 (4,5-dihydro-5-methyl-6-[4-[(2-methyl-3-oxo-1-cyclopentenyl) amino]phenyl]-3(2H)-pyridazinone), novel cardiotonic agents, were investigated in vitro and in vivo in comparison with those of other cardiotonic agents. In isolated guinea pig left atria, the positive inotropic EC50 values (microM) in order of potency were about 0.18 (NSP-805), 0.39 (indolidan), 1.1 (MCI-154), 1.7 (NSP-804, milrinone), 2.0 (denopamine), 4.0 (papaverine), 4.4 3-isobutyl-1-methylxanthine, IBMX, 6.5 (imazodan), and 27 (amrinone). In anesthetized dogs, intravenous (i.v.) injection of NSP-804 and NSP-805 produced 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 values (micrograms/kg) for LVdP/dtmax of NSP-804, NSP-805, denopamine, milrinone, MCI-154, and indolidan were 15, 12, 22, 23, 15, and 7.3, respectively. When the drugs were administered intraduodenally to anesthetized dogs, the ED50 values (micrograms/kg) for LVdP/dtmax of NSP-804, NSP-805, milrinone and indolidan were approximately 30, 10, 200, and 25 respectively. In the propranolol-induced heart failure model, NSP-804 and NSP-805 completely improved the hemodynamic state of heart failure to normal levels. The in vitro positive inotropic effects of NSP-804 and NSP-805 were accompanied by increases in tissue cyclic AMP and abolished by carbachol. NSP-805 was the most potent and selective inhibitor of guinea pig cardiac phosphodiesterase (PDE) III among the agents examined, and NSP-804 was a potent and selective inhibitor of PDE III similar to indolidan. The cardiovascular properties determined in this study suggest that both NSP-804 and NSP-805 may have beneficial effects for treatment of congestive heart failure (CHF).

[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.PMID:12420371doi

Purpose: To investigate the ocular effect of intravenous administration of a phosphodiesterase type 3 inhibitor (NSP-805) and to compare the effect of NSP-805 with that of a calcium antagonist (nicardipine hydrochloride) on chorio-retinal blood flow in anesthetized albino rabbits. Methods: Twenty-four female albino rabbits (weighting 2.0-4.0 kg) were anesthetized with intravenous injection. NSP-805(40 micrograms/kg and 100 micrograms/kg) and nicardipine of 40 micrograms/kg were intravenously administrated to the anesthetized rabbits. Intravenously administration of 20% dimethyl sulfoxide (DMSO) was used as a vehicle. Chorio-retinal blood flow was measured with a laser Doppler flowmeter at baseline and every 20 minutes after intravenous administration for 120 minutes. Heart rates and systemic blood pressure were monitored. Baseline measurements were compared with every 10 minutes after intravenous administration. Differences between the drug groups and vehicle group were analyzed. Results: After administration of a low dose of NSP--805 (40 micrograms/kg) and nicardipine (40 micrograms/kg), the chorio-retinal blood flow was significantly increased (p < 0.05). A high dose NSP-805(100 micrograms/kg) reduced systemic blood pressure significantly, but the increase of chorio-retinal blood flow was less than that at the low dose of NSP-805(40 micrograms/kg) and nicardipine (40 micrograms/kg). Chorio-retinal blood flow in the NSP 805(40 micrograms/kg) and nicardipine (40 micrograms/kg) groups was significantly increased over that in the control group (20% DMSO) (p < 0.05). Conclusion: The results suggest that the NSP-805 has the potential of increasing chorio-retinal blood flow in rabbit eyes.

Identification and characterization of isoenzymes of cyclic nucleotide phosphodiesterase in human kidney and heart, and the effects of new cardiotonic agents on these isoenzymes

Naunyn Schmiedebergs Arch Pharmacol 1994 Sep;350(3):284-93.PMID:7824045DOI:10.1007/BF00175034.

The present study was done to identify and characterize the isoenzymes of cyclic nucleotide phosphodiesterase (PDE) and to determine their intracellular distribution in human kidney and heart. The in vitro effects of new cardiotonic agents, namely, NSP-805 (4,5-dihydro-5-methyl-6-[4-[(2-methyl-3-oxo-1-cyclopentenyl)amino] phenyl]-3(2H)-pyridazinone), TZC-5665 (6-[4-[2-[3-(5-chloro-2-cyanophenoxy)-2-hydroxypropylamino]- 2 -methylpropylamino]phenyl]-5-methyl-4,5-dihydro-3(2H)-pyridazinone ) and its metabolites, OPC-18790 ((+/-)-6-[3-(3,4-dimethoxybenzylamino)-2 -hydroxypropoxy]-2-(1H)-quinolinone), MS-857 (4-acetyl-1-methyl-7-(4-pyridyl)-5,6,7,8-tetrahydro-3(2H)-isoquinolinone ) and E-1020 (1,2-dihydro-6-methyl-2-oxo-5-(imidazo[1,2-a]pyridin-6-yl)-3-pyridine carbonitrile hydrochloride monohydrate), on these human PDE isoenzymes were also investigated. PDE isoenzymes were separated from cytosolic and particulate fractions of homogenates of human kidney and heart by DEAE-Sepharose chromatography. PDE isoenzymes were identified by their elution characteristics, substrate specificities, sensitivities to regulation by effectors and by the use of isoenzyme-specific inhibitors. In a cytosolic fraction from kidney, Ca2+/calmodulin-dependent PDE (CaM-PDE), cyclic GMP-stimulated PDE (cGS-PDE), cyclic GMP-inhibited PDE (cGI-PDE) and two forms of cyclic AMP-specific PDE (cAMP-PDE) were resolved. One form of cAMP-PDE (cAMP-PDE alpha), which was eluted at a lower ionic strength than cGI-PDE during DEAE-Sepharose chromatography, was newly recognized in human tissues, though the other form (cAMP-PDE beta), which eluted later than cGI-PDE, had been previously isolated.(ABSTRACT TRUNCATED AT 250 WORDS)