Details
| Stereochemistry | UNKNOWN |
| Molecular Formula | C19H18N4O2.ClH |
| Molecular Weight | 370.833 |
| Optical Activity | ( - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.COC1=CC=C(C=C1)C2=NC3=C(N2)C=CC(=C3)C4=NNC(=O)CC4C
InChI
InChIKey=OJLOGBZTFKPHDQ-UHFFFAOYSA-N
InChI=1S/C19H18N4O2.ClH/c1-11-9-17(24)22-23-18(11)13-5-8-15-16(10-13)21-19(20-15)12-3-6-14(25-2)7-4-12;/h3-8,10-11H,9H2,1-2H3,(H,20,21)(H,22,24);1H
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C19H18N4O2 |
| Molecular Weight | 334.3718 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
DescriptionCurator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/1660359
Curator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/1660359
Pimobendan (INN, or pimobendane; tradenames Vetmedin, Acardi, and Heartmedin) is a veterinary medication. Under the trade name Acardi, it is available for human use in Japan. Usually, this medicine is used to treat acute heart failure and chronic heart failure (mild to moderate in severity). By increasing the calcium ion sensitivity to protein regulating myocardial contraction and also by inhibiting phosphodiesterase (PDE-III) activity, this medicine dilates the blood vessels and improves the symptoms of heart failure such as shortness of breath and difficulty in breathing. Pimobendan is metabolized into an active metabolite (desmethylpimobendan) by the liver. The parent compound, pimobendan, is a potent calcium sensitizer while desmethylpimobendan is a more potent phosphodiesterase III inhibitor. Pimobendan is 90–95% bound to plasma proteins in circulation. This may have implications in patients suffering from low blood protein levels (hypoproteinemia/hypoalbuminemia) and in patients that are on concurrent therapies that are also highly protein bound.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Differential modulation of cytokine production by drugs: implications for therapy in heart failure. | 1996 Dec |
|
| The novel insulinotropic mechanism of pimobendan: direct enhancement of the exocytotic process of insulin secretory granules by increased Ca2+ sensitivity in beta-cells. | 1998 Mar |
|
| Effect of pimobendan in patients with chronic heart failure. | 2001 Winter |
|
| [Roles of cytokines in the pathogenesis of heart failure]. | 2003 May |
|
| Investigation of pimobendan versus benazepril in canine myxomatous valvular disease. | 2003 Oct 4 |
|
| Do medical house officers value the health of veterans differently from the health of non-veterans? | 2004 Apr 7 |
|
| Successful allogeneic bone marrow transplantation for acute myelogenous leukemia after drug-induced cardiomyopathy. | 2004 Sep |
|
| Use of pimobendan in the management of heart failure. | 2004 Sep |
|
| Increased mitral valve regurgitation and myocardial hypertrophy in two dogs with long-term pimobendan therapy. | 2005 |
|
| [If the myofilaments become sensitive: Ca2+-sensitizer for the therapy of heart insufficiency]. | 2005 Apr 15 |
|
| Ca2+-sensitisers--a promising option to treat heart failure? | 2005 Dec |
|
| Selective blockade of nicotinic acetylcholine receptors by pimobendan, a drug for the treatment of heart failure: reduction of catecholamine secretion and synthesis in adrenal medullary cells. | 2005 Feb |
|
| [Cytokine antagonists and endothelin antagonists for therapy of heart failure]. | 2005 Feb 10 |
|
| Pharmacokinetic characterization of transcellular transport and drug interaction of digoxin in Caco-2 cell monolayers. | 2005 Jan |
|
| Efficacy and safet of pimobendan in canine heart failure caused by myxomatous mitral valve disease. | 2005 Mar |
|
| Effect of pimobendan on cardiopulmonary baroreflex control of sympathetic nerve activity in healthy young men. | 2005 Oct 30 |
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| A review of levosimendan in the treatment of heart failure. | 2006 |
|
| Pimobendan in heart failure therapy--a silver bullet? | 2006 Mar-Apr |
|
| New insights in the treatment strategy for pulmonary arterial hypertension. | 2006 Oct |
|
| Beta-blockers use in patients with chronic obstructive pulmonary disease and concomitant cardiovascular conditions. | 2007 |
|
| Effects of pimobendan for mitral valve regurgitation in dogs. | 2007 Apr |
|
| [Combined therapy with weight loss and amiodarone improved cardiac function in a patient with idiopathic dilated cardiomyopathy complicated with severe obesity: a case report]. | 2007 Aug |
|
| A pilot study to assess the feasibility of a submaximal exercise test to measure individual response to cardiac medication in dogs with acquired heart failure. | 2007 Aug |
|
| Knock-in mouse model of dilated cardiomyopathy caused by troponin mutation. | 2007 Jul 20 |
|
| [Calcium sensitizer agents in heart failure therapy]. | 2007 May 28 |
|
| Treatment options in myocarditis: what we know from experimental data and how it translates to clinical trials. | 2007 Sep |
|
| The value added by measuring myocardial contractility 'in vivo' in safety pharmacological profiling of drug candidates. | 2007 Sep-Oct |
|
| Effect of short-term treatment with meloxicam and pimobendan on the renal function in healthy beagle dogs. | 2008 Apr |
|
| Cardiac Ca2+ signaling and Ca2+ sensitizers. | 2008 Dec |
|
| Defining the binding site of levosimendan and its analogues in a regulatory cardiac troponin C-troponin I complex. | 2008 Jul 15 |
|
| The role of cardiac troponin T quantity and function in cardiac development and dilated cardiomyopathy. | 2008 Jul 9 |
|
| Effect of pimobendan on case fatality rate in Doberman Pinschers with congestive heart failure caused by dilated cardiomyopathy. | 2008 Jul-Aug |
|
| Anaesthesia for the geriatric dog and cat. | 2008 Jun 1 |
|
| Validity, reliability, and responsiveness of the Kansas City Cardiomyopathy Questionnaire in anemic heart failure patients. | 2008 Mar |
|
| Concerns about "Comparative adverse cardiac effects of pimobendan and benazepril monotherapy in dogs with mild degenerative mitral valve disease". | 2008 Mar-Apr |
|
| Concerns about "Comparative adverse cardiac effects of pimobendan and benazepril monotherapy in dogs with mild degenerative mitral valve disease: a prospective, controlled, blinded and randomized study". | 2008 Mar-Apr |
|
| Alterations in vasomotor control of coronary resistance vessels in remodelled myocardium of swine with a recent myocardial infarction. | 2008 May |
|
| Canine heart disease: progress and promise. | 2008 Nov |
|
| Effect of pimobendan or benazepril hydrochloride on survival times in dogs with congestive heart failure caused by naturally occurring myxomatous mitral valve disease: the QUEST study. | 2008 Sep-Oct |
|
| Agents with inotropic properties for the management of acute heart failure syndromes. Traditional agents and beyond. | 2009 Dec |
|
| Sarcomere control mechanisms and the dynamics of the cardiac cycle. | 2010 |
|
| Canine dilated cardiomyopathy: a retrospective study of prognostic findings in 367 clinical cases. | 2010 Aug |
|
| Patients' self-assessed functional status in heart failure by New York Heart Association class: a prognostic predictor of hospitalizations, quality of life and death. | 2010 Feb |
|
| Synthesis of new 4,5-3(2H)pyridazinone derivatives and their cardiotonic, hypotensive, and platelet aggregation inhibition activities. | 2010 Jan |
|
| Human cardiac tissue in a microperfusion chamber simulating extracorporeal circulation--ischemia and apoptosis studies. | 2010 Jan 18 |
|
| Canine degenerative myxomatous mitral valve disease: natural history, clinical presentation and therapy. | 2010 Jul |
|
| Current use of pimobendan in canine patients with heart disease. | 2010 Jul |
|
| Synthesis, vasorelaxant activity and antihypertensive effect of benzo[d]imidazole derivatives. | 2010 Jun 1 |
|
| ECG of the month. Arrhythmogenic right ventricular cardiomyopathy in a Boxer. | 2010 May 1 |
|
| Refining the human iPSC-cardiomyocyte arrhythmic risk assessment model. | 2013 Dec |
Sample Use Guides
Acute heart failure: usually for adults, one capsule (2.5 mg of pimobendan) once daily
Chronic heart failure (mild to moderate in severity): usually for adults, one capsule (2.5 mg of pimobendan) twice daily after meals
Route of Administration:
Oral
composite platelet aggregation (area under the curve [AUC]) and maximal platelet aggregation (aggregation units [AUs]) at 10.0μM pimobendan were significantly decreased for collagen-induced aggregation (AUC, 349.7 ± 58.4 vs 285.1 ± 72.2; maximal platelet aggregation, 196.2 ± 25.8 AUs vs 161.5 ± 38.0 AUs), and the AUC and velocity of aggregation at 10.0μM pimobendan were significantly decreased for ADP-induced aggregation (AUC, 268.5 ± 35.1 vs 213.4 ± 77.2; velocity of aggregation, 15.7 ± 2.9 AUs/min vs 11.8 ± 3.5 AUs/min).
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:20:46 GMT 2023
by
admin
on
Sat Dec 16 11:20:46 GMT 2023
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| Record UNII |
E57W8B5UBF
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| Record Status |
Validated (UNII)
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| Record Version |
|
-
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E57W8B5UBF
Created by
admin on Sat Dec 16 11:20:46 GMT 2023 , Edited by admin on Sat Dec 16 11:20:46 GMT 2023
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RACEMATE -> ENANTIOMER |
