Pimobendan

• CAT Number: A000555
• CAS Number: 74150-27-9
• Molecular Formula: C19H18N4O2
• Molecular Weight: 334.379
• Purity: ≥95%
• Target: PDE
• Solubility: >16.2mg/mL in DMSO
• Storage: -20°C
• IUPAC Name: 3-[2-(4-methoxyphenyl)-3H-benzimidazol-5-yl]-4-methyl-4,5-dihydro-1H-pyridazin-6-one
• InChI: InChI=1S/C19H18N4O2/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)
• InChIKey: GLBJJMFZWDBELO-UHFFFAOYSA-N
• SMILES: CC1CC(=O)NN=C1C2=CC3=C(C=C2)N=C(N3)C4=CC=C(C=C4)OC

Pimobendan (CAS 74150-27-9) is a veterinary medication. Pimobendan is both a calcium sensitizer and a selective inhibitor of phosphodiesterase III (PDE3) with positive inotropic and vasodilator effects. Pimobendan is used in the management of heart failure in dogs, most commonly caused by myxomatous mitral valve disease (also previously known as endocardiosis), or dilated cardiomyopathy.Research has shown that pimobendan increases survival time and improves quality of life in canine patients with congestive heart failure secondary to mitral valve disease when compared with benazepril, an angiotensin-converting-enzyme (ACE) inhibitor.

Reference

1: Murphy LA, Russell N, Bianco D, Nakamura RK. Retrospective evaluation of pimobendan and sildenafil therapy for severe pulmonary hypertension due to lung disease and hypoxia in 28 dogs (2007-2013). Vet Med Sci. 2017 Mar 8;3(2):99-106. doi: 10.1002/vms3.60. eCollection 2017 May. PubMed PMID: 28713578; PubMed Central PMCID: PMC5488247.
2: King JN, Hirakawa A, Sonobe J, Otaki H, Sakakibara N, Seewald W, Forster S. Evaluation of a fixed dose combination of benazepril and pimobendan in dogs with congestive heart failure; a randomized non-inferiority clinical trial. J Vet Sci. 2017 Jul 10. [Epub ahead of print] PubMed PMID: 28693297.
3: Kuntz EA, Strehlau G, Giraudel JM, King JN. Safety of a benazepril and pimobendan combination tablet in adult healthy dogs. J Vet Pharmacol Ther. 2017 Jun 26. doi: 10.1111/jvp.12423. [Epub ahead of print] PubMed PMID: 28649790.
4: Kreibich M, Berchtold-Herz M, Beyersdorf F, Trummer G. Pimobendan in Chronic Right Heart Failure in a Left Ventricular Assist Device Patient. Thorac Cardiovasc Surg Rep. 2016 Dec;5(1):39-40. doi: 10.1055/s-0036-1571286. Epub 2016 Jan 29. PubMed PMID: 28018821; PubMed Central PMCID: PMC5177432.
5: Yata M, McLachlan AJ, Foster DJ, Hanzlicek AS, Beijerink NJ. Single-dose pharmacokinetics and cardiovascular effects of oral pimobendan in healthy cats. J Vet Cardiol. 2016 Dec;18(4):310-325. doi: 10.1016/j.jvc.2016.07.001. Epub 2016 Sep 6. PubMed PMID: 27613648.
6: Boswood A, Häggström J, Gordon SG, Wess G, Stepien RL, Oyama MA, Keene BW, Bonagura J, MacDonald KA, Patteson M, Smith S, Fox PR, Sanderson K, Woolley R, Szatmári V, Menaut P, Church WM, O/'Sullivan ML, Jaudon JP, Kresken JG, Rush J, Barrett KA, Rosenthal SL, Saunders AB, Ljungvall I, Deinert M, Bomassi E, Estrada AH, Fernandez Del Palacio MJ, Moise NS, Abbott JA, Fujii Y, Spier A, Luethy MW, Santilli RA, Uechi M, Tidholm A, Watson P. Effect of Pimobendan in Dogs with Preclinical Myxomatous Mitral Valve Disease and Cardiomegaly: The EPIC Study-A Randomized Clinical Trial. J Vet Intern Med. 2016 Nov;30(6):1765-1779. doi: 10.1111/jvim.14586. Epub 2016 Sep 28. PubMed PMID: 27678080; PubMed Central PMCID: PMC5115200.
7: Mizuno M, Yamano S, Chimura S, Hirakawa A, Takusagawa Y, Sawada T, Maetani S, Takahashi A, Mizuno T, Harada K, Shinoda A, Uchida S, Takeuchi J, Mizukoshi T, Endo M, Uechi M. Efficacy of pimobendan on survival and reoccurrence of pulmonary edema in canine congestive heart failure. J Vet Med Sci. 2017 Jan 20;79(1):29-34. doi: 10.1292/jvms.16-0069. Epub 2016 Sep 17. PubMed PMID: 27644192; PubMed Central PMCID: PMC5289233.
8: Apple SM, Menciotti G, Braz-Ruivo L, Crosara S, Häggström J, Borgarelli M. Effects of pimobendan on myocardial perfusion and pulmonary transit time in dogs with myxomatous mitral valve disease: a pilot study. Aust Vet J. 2016 Sep;94(9):324-8. doi: 10.1111/avj.12480. PubMed PMID: 27569835.
9: Jackson AE. In this issue – September 2016: Portable negative pressure wound therapy for skin grafts in dogs · Wellness testing in small animals · Effects of pimobendan on myocardial perfusion and pulmonary transit time in dogs · Rispens CVI988 vaccine virus and Marek/'s disease virus in poultry · A field study of ovulation in oestrus mares · Post-weaning growth of beef heifers. Aust Vet J. 2016 Sep;94(9):305-6. doi: 10.1111/avj.12484. PubMed PMID: 27569831.
10: Miyagawa Y, Machida N, Toda N, Tominaga Y, Takemura N. Comparison of the effects of long-term pimobendan and benazepril administration in normal cats. J Vet Med Sci. 2016 Aug 1;78(7):1099-106. doi: 10.1292/jvms.14-0673. Epub 2016 Mar 14. PubMed PMID: 26972332; PubMed Central PMCID: PMC4976264.