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Product Details
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Biological Activity |
Pimobendan is an inhibitor of phosphodiesterase 3 (PDE3; IC50 = 0.32 μM for guinea pig cardiac enzyme) that is selective for PDE3 over PDE1, PDE2, and PDE4 (IC50s = >30 μM). It is also a calcium sensitizer, decreasing the concentration of calcium required for half-maximal contractile force in isolated, skinned porcine ventricular fibers. Pimobendan increases the force of contraction in electrically-stimulated isolated guinea pig papillary muscles with an EC50 value of 6 μM, indicating positive inotropic effects. It increases survival time in dogs with congestive heart failure due to myxomatous mitral valve disease when administered in combination with angiotensin-converting enzyme inhibitors and furosemide . Formulations containing pimobendan have been used in the treatment of heart failure in dogs. |
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Biochem/physiol Actions |
Pimobendan is an inotropic agent with a dual mechanism of action: it increases myocardial contractility by increasing calcium sensitization to troponin C and it promotes vasodilation by inhibiting phosphodiesterase III (PDE3). Pimobendan has been studied for treating heart failure and cardiomyopathy, primarily for veterinary uses. |
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Veterinary Drugs and Treatments |
Pimobendan is used to treat dogs with congestive heart failure secondary to dilated cardiomyopathy or chronic mitral valve insufficiency (CMVI). |
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Definition |
ChEBI: Pimobendan is a pyridazinone and a member of benzimidazoles. It has a role as a cardiotonic drug, a vasodilator agent and an EC 3.1.4.* (phosphoric diester hydrolase) inhibitor. |
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Brand name |
Acardl |
InChI:InChI=1/C19H18N4O2/c1-11-9-16(22-23-19(11)24)13-5-8-15-17(10-13)21-18(20-15)12-3-6-14(25-2)7-4-12/h3-8,10-11H,9H2,1-2H3,(H,20,21)(H,23,24)/t11-/m1/s1
The invention relates to a novel prepara...
The invention provides a synthesis metho...
The invention discloses a novel method f...
The invention discloses a chemical synth...
(5RS)-6-[1-(4-methoxybenzyl)-2-(4-methoxyphenyl)-1H-benzimidazole-6-yl]-5-methyl-4,5-dihydro-3(2H)pyridazinone
pimobendan
| Conditions | Yield |
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With ammonium cerium (IV) nitrate; In water; acetone; at 20 ℃; for 3h; Temperature;
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91% |
6-(2-bromo-1H-benzo[d]imidazol-6-yl)-5-methyl-4,5-dihydropyridazin-3(2H)-one
2-(4-methoxyphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane
pimobendan
| Conditions | Yield |
|---|---|
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6-(2-bromo-1H-benzo[d]imidazol-6-yl)-5-methyl-4,5-dihydropyridazin-3(2H)-one; With caesium carbonate; In 1,4-dioxane; N,N-dimethyl-formamide; at 20 ℃; for 1h; Inert atmosphere;
2-(4-methoxyphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane; With bis-triphenylphosphine-palladium(II) chloride; In 1,4-dioxane; N,N-dimethyl-formamide; at 80 - 85 ℃; for 12h; Inert atmosphere;
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84.9% |
4-chlorobenzaldehyde
6-(4-chloro-3-nitrophenyl)-5-methyl-2,3,4,5-tetrahydropyridazin-3-one
4-methoxy-benzaldehyde
6-(3,4-diaminophenyl)-5-methyl-2,3,4,5-tetrahydropyridazin-3-one
4,5-dihydro-6-(2-(4-methoxyphenyl)-1H-benzimidazol-5-yl)-5-methyl-3(2H)-pyridazinone hydrochloride
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