7434. Pimobendan

Nomenclature

CAS number: 74150-27-9
4,5-Dihydro-6-[2-(4-methoxyphenyl)-1H-benzimidazol-5-yl]-5-methyl-3(2H)-pyridazinone; UD-CG 115; UD-CG 115 BS; 2-(4-methoxyphenyl)-5(6)-(5-methyl-3-oxo-4,5-dihydro-2H-6-pyridazinyl)benzimidazole; Acardi (Boehringer, Ing.); Vetmedin (Boehringer, Ing.).
C19H18N4O2; mol wt 334.37.
C 68.25%, H 5.43%, N 16.76%, O 9.57%.

Description and references

Positive inotropic agent. Prepn: V. Austel et al., DE 2837161; eidem, US 4361563 (1980, 1982 both to Thomae). Cardiovascular effects: J. C. A. von Meel, Arzneim.-Forsch. 35, 284 (1985); P. D. Verdouw et al., Eur. J. Pharmacol. 126, 21 (1986). Comparison of enantiomer activity: K. Fujino et al., J. Pharmacol. Exp. Ther. 247, 519 (1988). HPLC determn of enantiomers in plasma: M. Asakura et al., J. Chromatogr. 614, 135 (1993). Clinical trial in congestive heart failure: F. Hagemeijer, Am. Heart J. 122, 517 (1991); S. D. Katz et al., ibid. 123, 95 (1992). Clinical pharmacokinetics and pharmacodynamics: K.-M. Chu et al., Drug Metab. Dispos. 27, 701 (1999). Veterinary use in heart failure: V. L. Fuentes, Vet. Clin. North Am. Small Anim. Pract. 34, 1145 (2004). Review of pharmacology and therapeutic potential: A. Fitton, R. N. Brogden, Drugs Aging 4, 417-441 (1994).

Chemical structure

Derivative

Hydrochloride.

Nomenclature

CAS number: 77469-98-8
C19H18N4O2.HCl; mol wt 370.83.
C 61.54%, H 5.16%, N 15.11%, O 8.63%, Cl 9.56%.

Properties

Crystals from methanol and ethereal HCl, mp 311°(dec). LD50 orally in mice: ≈600 mg/kg (Austel, 1982).

Therapeutic Category

Cardiotonic.

Therapeutic Category (Veterinary)

Cardiotonic.

Keywords

Cardiotonic