Details
Stereochemistry | ACHIRAL |
Molecular Formula | C11H11N3O2 |
Molecular Weight | 217.2239 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCC1=C(NC(=O)N1)C(=O)C2=CC=NC=C2
InChI
InChIKey=OQGWJZOWLHWFME-UHFFFAOYSA-N
InChI=1S/C11H11N3O2/c1-2-8-9(14-11(16)13-8)10(15)7-3-5-12-6-4-7/h3-6H,2H2,1H3,(H2,13,14,16)
Piroximone is a nonglycoside, noncatecholamine inotropic agent. In animal experiments, it has been shown to increase cardiac contractility by mechanisms unrelated to any known receptor, acting mainly by inhibition of type III phosphodiesterase. Piroximone also possesses direct vasodilatory properties in the arterial and venous vascular bed. Piroximone combines well-balanced vasodilator and inotropic properties which make it very useful for the management of congestive heart failure. Piroximone had been in phase II clinical trial for the treatment of heart failure. However, this research has been discontinued.
Originator
Approval Year
PubMed
Title | Date | PubMed |
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Studies on the mechanism of the cardiotonic activity of MDL 19205: effects on several biochemical systems. | 1984 Jan-Feb |
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Acute hemodynamic effects of MDL 19205 in mild congestive heart failure. | 1987 Feb |
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The influence of clinical intervention on pressure-volume relationships--the conductance (volume) technique. | 1992 Nov |
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Comparison of the haemodynamic effects of enoximone and piroximone in patients after cardiac surgery. | 1993 Dec |
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Hemodynamic effects and concentration-effect relationship of a graded infusion of piroximone in patients with severe heart failure. | 1993 Mar |
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Circulatory effects of the PDE-inhibitors piroximone and enoximone. | 1993 Oct |
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Postischemic hemodynamic changes after piroximone administration in isolated rabbit heart. | 1994 |
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Additive haemodynamic effects of piroximone and prostacyclin in severe chronic heart failure. | 1994 Apr |
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[Continuous monitoring of cardiac output by analysis of the pulse contour]. | 1994 Jan |
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Effects of piroximone on the right ventricular function in severe heart failure patients. | 1994 May |
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Determination of piroximone in human plasma by high-performance liquid chromatography. | 1994 Oct |
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Pharmacokinetics of piroximone after oral and intravenous administration to patients with renal insufficiency. | 1995 Feb |
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Metabolism and pharmacokinetics of the cardiotonic agent piroximone and of its major metabolite in dog. | 1995 Jan |
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Direct depressant effect of phosphodiesterase inhibitors on ATPase activity of rat cardiac myofibrils. | 1995 May |
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Synergistic interaction of adenylate cyclase activators and nitric oxide donor SIN-1 on platelet cyclic AMP. | 1995 May 26 |
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[Acute hemodynamic effects of piroximone i.v. in patients with severe heart failure]. | 1995 Oct |
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Preischemic bolus application of piroximone studied on the isolated rabbit heart--a second look including biochemical data. | 1996 |
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Phosphodiesterase inhibitors piroximone and enoximone inhibit platelet aggregation in vivo and in vitro. | 1997 Oct 15 |
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Clinical pharmacokinetics of vasodilators. Part II. | 1998 Jul |
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A comparison of the inotropic effects of milrinone and piroximone. | 2001 Jan |
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Therapeutic benefit of pentostatin in severe IL-10-/- colitis. | 2008 Jul |
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Real-time concurrent monitoring of apoptosis, cytosolic calcium, and mitochondria permeability transition for hypermulticolor high-content screening of drug-induced mitochondrial dysfunction-mediated hepatotoxicity. | 2012 Oct 17 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2419699
Single dose - 1 mg/kg
Route of Administration:
Intravenous
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C744
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C90921
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55263
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C039686
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2VSD0380YB
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CHEMBL58355
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84490-12-0
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SUB09938MIG
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U-82
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)