Details
Stereochemistry | ACHIRAL |
Molecular Formula | C14H10N4O |
Molecular Weight | 250.2554 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C(C=C(C#N)C(=O)N1)C2=CN3C=CN=C3C=C2
InChI
InChIKey=JPAWFIIYTJQOKW-UHFFFAOYSA-N
InChI=1S/C14H10N4O/c1-9-12(6-11(7-15)14(19)17-9)10-2-3-13-16-4-5-18(13)8-10/h2-6,8H,1H3,(H,17,19)
DescriptionSources: http://www.ncbi.nlm.nih.gov/pubmed/2566308Curator's Comment: description was created based on several sources, including
http://www.eisai.jp/medical/products/di/EPI/COR_A_EPI.pdf
Sources: http://www.ncbi.nlm.nih.gov/pubmed/2566308
Curator's Comment: description was created based on several sources, including
http://www.eisai.jp/medical/products/di/EPI/COR_A_EPI.pdf
Olprinone (INN) is a cardiotonic agent, is used for treatment acute heart failure. It has been marketed in Japan since 1996. The main mechanism of action of olprinone hydrochloride hydrate is selective inhibition of PDE III specific to cAMP. It is considered that this action causes an increase in intracellular cAMP levels and peak Ca2+ levels, thereby increasing myocardial contractility.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL2094125 Sources: http://www.ncbi.nlm.nih.gov/pubmed/2566308 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
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Effects of olprinone, a phosphodiesterase 3 inhibitor, on regional cerebral blood flow of cerebral cortex in stroke patients. | 2001 Apr |
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Use of olprinone, a phosphodiesterase III inhibitor, in an asthmatic patient. | 2001 Apr |
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Effects of olprinone, a new phosphodiesterase inhibitor, on gastric intramucosal acidosis and systemic inflammatory responses following hypothermic cardiopulmonary bypass. | 2001 Apr |
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Cardioprotective effect afforded by transient exposure to phosphodiesterase III inhibitors: the role of protein kinase A and p38 mitogen-activated protein kinase. | 2001 Aug 7 |
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A comparison of the relaxant effects of olprinone and aminophylline on methacholine-induced bronchoconstriction in dogs. | 2001 Jul |
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The effects of olprinone (a phosphodiesterase III inhibitor) on hepatic vascular bed in a porcine model of endotoxemia. | 2001 Mar |
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Effect of phosphodiesterase III inhibitor on contractility, afterload, and vascular capacitance during right heart bypass preparation. | 2001 Oct |
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Olprinone: a phosphodiesterase III inhibitor with positive inotropic and vasodilator effects. | 2002 Fall |
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Effect of phosphodiesterase III inhibitor on plasma concentrations of endothelin-1 and tumour necrosis factor in patients with acute heart failure. | 2002 Feb |
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Inhaled olprinone improves contractility of fatigued canine diaphragm. | 2002 Mar |
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[Effects of olprinone hydrochloride on intraocular pressure and ocular blood flow in patients after cardiac surgery under cardiopulmonary bypass]. | 2002 Nov |
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Possible contribution of acetylamrinone and its enhancing effects on platelet aggregation under shear stress conditions in the onset of thrombocytopenia in patients treated with amrinone. | 2003 |
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Olprinone, a phosphodiesterase III inhibitor, does not affect hypoxia-induced pial arteriolar dilatation in rabbits. | 2003 Feb |
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Toborinone and olprinone, phosphodiesterase III inhibitors, inhibit human platelet aggregation due to the inhibition of both calcium release from intracellular stores and calcium entry. | 2004 |
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The phosphodiesterase III inhibitor olprinone decreases sensitivity of rat Kupffer cells to endotoxin. | 2004 Aug |
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Olprinone improves diaphragmatic contractility and fatigability during abdominal sepsis in a rat model. | 2004 May |
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Effects of olprinone on hepatosplanchnic circulation and mitochondrial oxidation in a porcine model of endotoxemia. | 2005 |
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Phosphodiesterase 3 inhibition and cough in elderly asthmatics. | 2005 Nov 24 |
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Vasoactive drugs and the gut: is there anything new? | 2006 Apr |
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Effects of olprinone on myocardial ischemia-reperfusion injury in dogs. | 2006 Aug |
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The enhancement of cellular cAMP with olprinone protects autotransplanted rat kidney against cold ischemia-reperfusion injury. | 2006 Jun |
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Effects of dopamine and olprinone on ventricular energetics in sevoflurane-induced acute left ventricular depression in dogs. | 2006 Jun |
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Metabolic effects of phosphodiesterase III inhibitors: another reason to promote their use? | 2007 |
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[Phosphodiesterase III inhibitor--characteristics, mechanisms of action, pharmacokinetics, indications, contraindications, clinical trials, and side effects]. | 2007 May 28 |
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[Anesthetic management of coronary artery bypass grafting for unstable angina pectoris in a patient undergoing home oxygen therapy]. | 2008 Apr |
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Pharmacological preconditioning in type 2 diabetic rat hearts: the roles of mitochondrial ATP-sensitive potassium channels and the phosphatidylinositol 3-kinase-Akt pathway. | 2009 Aug |
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[A case report of anesthesia for a child with Pompe's disease (glycogen storage disease type II)]. | 2009 Feb |
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[Use of cardiovascular drugs for cardiac surgery--based on recent studies]. | 2009 Mar |
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A phosphodiesterase III inhibitor protects rat liver from sinusoidal obstruction syndrome through heme oxygenase-1 induction. | 2009 May |
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Local application of olprinone for promotion of peripheral nerve regeneration. | 2009 Nov |
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A phosphodiesterase III inhibitor protects rat liver from sinusoidal obstruction syndrome through heme oxygenase-1 induction. | 2010 Apr |
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Anesthetic management of a patient undergoing liver transplantation who had previous coronary artery bypass grafting using an in situ right gastroepiploic artery. | 2010 Apr |
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Effect of olprinone, a phosphodiesterase III inhibitor, on hepatic ischemia-reperfusion injury in rats. | 2010 Apr |
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Differential vasodilation response to olprinone in rabbit renal and common carotid arteries. | 2010 Feb |
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[Right heart failure during modified ultrafiltration in pediatric living donor lobar lung transplantation]. | 2010 Feb |
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Olprinone attenuates the development of ischemia/reperfusion injury of the gut. | 2010 Jul |
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The effects of the phosphodiesterase inhibitor olprinone on global cerebral ischemia. | 2010 Mar 1 |
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Ethyl 8-(4-nitro-phen-yl)imidazo[1,2-a]pyridine-7-carboxyl-ate. | 2010 Nov 24 |
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Olprinone attenuates the acute inflammatory response and apoptosis after spinal cord trauma in mice. | 2010 Sep 7 |
Patents
Sample Use Guides
intravenously at a dose of 10 µg/kg of olprinone hydrochloride hydrate, gradually over 5
min, and then drip-infused intravenously at a rate of 0.1 - 0.3 µg/kg/min
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/7736650
E-1020 (Olprinone) may improve diastolic function as well as systolic function in failing hearts. Effects of E-1020, on intracellular calcium transients were compared with those of isoproterenol (ISO) in isolated single myocytes from failing hearts secondary to pulmonary hypertension induced by monocrotaline injection. Myocytes were isolated by enzyme digestion using a Langendorff apparatus. Changes in intracellular calcium concentrations ([Ca2+]i) were recorded using a fura-2 fluorescence microscopic technique.
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NCI_THESAURUS |
C744
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1987
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C059498
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CHEMBL1474900
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SUB09434MIG
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DTXSID1048461
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C90918
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4593
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7123
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OLPRINONE
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100000083335
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m6902
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106730-54-5
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4Y8BMI9YGC
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)