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CasNo： 74150-27-9
MF： C19H18N4O2
| Description | Pimobendan is effective in treatment of dogs with congestive heart failure (CHF) secondary to myxomatous mitral valve disease (MMVD). |
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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. |
| Factory / Manufacturer | Liaoning Pharmaceutical Innovation Co.,Ltd. was registered on September 16, 2021, with a registered capital of 12 million. It is located in Panjin Fine Chemical Industrial Park, Liaoning. It is an enterprise integrating the development, research and production of raw materials and intermediate processes. Our company's main business covers all over the world. We have 47 patents including 6 authorized invention patents . The company has been recognized as a national high-tech enterprise and has established a quality management system with ISO9000 and ICHQ7 as the core, ISO14001 international environmental management certification system and OHSAS18001 occupational health management system. |
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 use of pimobendan, an inodilator with phosphodiesterase 3 (PDE3) inhibitory and calcium-sensitizing properties, is regarded as a component of the standard of care in the management of dogs with CHF secondary to both DCM and CVHD. Further studies are warranted to confirm the safety and efficacy of pimobendan for the off-label use of this drug in asymptomatic CVHD, pulmonary arterial hypertension, asymptomatic myocardial diseases, CHF from all other causes and in cats with CHF.
Hazard ratio for the pimobendan group was 0.64 (95% CI: 0.47–0.87) compared with the placebo group. The benefit persisted after adjustment for other variables. Adverse events were not different between treatment groups. Dogs in the pimobendan group lived longer (median survival time was 1059 days (95% CI: 952–NA) in the pimobendan group and 902 days (95% CI: 747–1061) in the placebo group) (P = .012).
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](/upload/2024/11/f14a45f5-abd3-459a-96d3-d2bbca6fdb5a.png)
(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](/upload/2024/11/23794398-d1e7-423d-98b6-afc38bd4731a.png)
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
Address：No.20 Building, Area A ,Park Street South, Industry & Trade Road West Industrial Park, Shuangtaizi District, Panjin City, Liaoning Province,ChinaEmail：lancy@pipharma.com.cn;sales@pipharma.com.cn
Tel：022-66350830Phone：13322388077/+86-16588669988
