Reversal of phosphate induced decreases in force by the benzimidazole pyridazinone, UD-CG 212 CL, in myofilaments from human ventricle

Molecular and Cellular Biochemistry

Volumn 176, Issue 1-2, 1997, Pages 83-88

  Fraker, Lesa D ^a   Eyk, Van Jennifer ^b   Solaro, R John ^b  

^a Department of Emergency Medicine ^*  (United States)

^b UNIVERSITY OF ILLINOIS   (United States)

Author keywords

Calcium sensitivity; Heart failure; Pimobendan; Skinned fiber bundles

Indexed keywords

ADENOSINE TRIPHOSPHATE MAGNESIUM; BENZIMIDAZOLE; CALCIUM ION; O NORPIMOBENDAN; PHOSPHATE; PIMOBENDAN; PYRIDAZINONE DERIVATIVE;

ARTICLE; CONTROLLED STUDY; HEART VENTRICLE; HUMAN; HUMAN CELL; HUMAN TISSUE; MYOFILAMENT;

CALCIUM; CARDIOTONIC AGENTS; HEART; HEART VENTRICLES; HUMANS; MICROFILAMENTS; MYOCARDIAL CONTRACTION; PHOSPHATES; PYRIDAZINES;

EID: 0030810117     PISSN: 03008177     EISSN: None     Source Type: Journal    
DOI: 10.1023/A:1006827012495     Document Type: Article

References (19)

1. Ruegg JC, Solaro RJ: Calcium sensitizing positive inotropic drugs. In: JK Gwathmey, GM Briggs, PD Allen (eds). Heart Failure Basic and Clinical Aspects. Marcel Dekker, Inc., New York, 1993, pp. 457-477
2. Ruegg JC, Pfitzer G, Eubler D, Zeugner C: Effect on contractility of skinned fibers from mammalian heart and smooth muscle by a new benzimidazole derivative,4,5-Dihydro-6-[2-(4-methoxyphenyl)-1H-benzimidazole-5-yl]-5-methyl-3 (2H)-pyridazinone. Arzneim-Forsch/Drug Res 34: 1736-1738, 1984
3. Solaro RJ, Gambassi G, Warshaw DM, Keller MR, Spurgeon HA, Beier N, Lakatta EG: Steroselective actions of thiadiazinones on dog cardiac myocytes and myofilaments. Circ Res 73: 981-990, 1993
4. 2+-sensitivity of cardiac myofibrils and sarcoplasmic reticulum in guinea pig heart. Circ Res 77: 107-113, 1995
5. Wolska BM, Kitada Y, Palmiter KA, Westfall M., Johnson MD, Solaro RJ: CGP48506, a novel benzodiazocine derivative, increases contractility of ventricular myocytes and myofilaments by direct effects on the actin-myosin reaction. Am J Physiol (Heart) 270: H24, 1996
6. Hagemeijer F, Roth W, Brand HJ: Correlations between the cardiovascular effects of pimobendan and plasma concentrations of the parent compound and of its major active metabolite, UD-CG 12 Cl, in patients with congestive heart failure. J Cardiovasc Pharmacol 14: S57-S64, 1989
7. Kubo SH, Gollub S, Bourge R, Rahko P, Cobb F, Jessup M, Brozena S, Brodsky M, Kirlin P, Shanes J, Konstarn M, Gradman A, Morledge J, Cinquegrani M, Singh S, LeJemtel T, Nicklas J, Troha J, Cohn JN: Beneficial effects of pimobendan on exercise tolerance and quality of life in patients with heart failure. Results of a multicenter trial. Circ 85: 942-949, 1992
8. Katz SD, Kubo SH, Jessup M, Brozena S, Troha JM, Wahl J, Cohn JN, Sonneblick MD, LeJemtel TH: A multicenter, randomized, double-blind, placebo-controlled trial of pimobendan, a new cardiotonic and vasodilator agent, in patients with severe congestive heart failure. Am Heart J 123: 95-102, 1992
9. 2+-activation and the inotropic effect of pimobendan: comparison with milrinone. Circ Res 63: 911-922, 1988
10. Brunhorst B, van der Leyen H, Meter W, Nigbur R, Schmidt-Schumacher C, Scholtz H: Relation of positive inotropic and chronotropic effects of pimobendan, UD-CG 212 Cl, milrinone and other phosphodiesterase inhibitors to phosphodiesterase III inhibition in guinea-pig heart. Naunyn-Schmiedeberg's Arch Pharmacol 339: 575-583, 1989
11. Solaro RJ, Fujino K, Sperelakis N: The positive inotropic effect of pimobendan involves stereospecific increases in the calcium sensitivity of cardiac myofilaments. J Cardiovasc Pharmacol 14: S7-S12, 1989
12. Bohm M, Morano I, Pieske B, Ruegg JC, Wankerl M, Zimmerman R, Erdmann E: Contribution of cAMP-phosphodiesterase inhibition and sensitization of the contractile proteins for calcium to the inotropic effect of pimobendan in the failing human myocardium. Circ Res 68: 689-701, 1991
13. Endoh M, Shibasaki T, Satoh H, Norota I, Ishihata A: Different mechanism involved in the positive inotropic effects of benzimidazole derivative UD-CG 115 BS (pimobendan) and its demethylated metabolite UD-CG 212 Cl in canine ventricular myocardium. J Cardiovasc Pharmacol 17: 365-375, 1991
14. Van Meel JCA, Redemann N, Diederen W, Haigh RM: Low concentrations of UD-CG 212 enhance myocyte contractility by an increase in calcium responsiveness in the presence of inorganic phosphate. Naunyn-Schmiedeberg's Arch Pharmacol 351: 644, 1995
15. Komukai K, Kurihara S: Mechanisms of the inotropic effects of UDCG 212 Cl, an active metabolise of pimobendan, on ferret papillary muscles. J Cardiovasc Pharmacol 27: 673-679, 1996
16. Westfall MV, Wahler GM, Solaro RJ: A highly specific benzimidazole pyridazinone reverses phosphate-induced changes in cardiac myofilament activation. Biochem 32: 10464-10470, 1993
17. Allen DG, Morris PG, Orchard CH, Parol J: A nuclear magnetic resonance study of metabolism in the ferret heart during hypoxia and inhibition of glycolysis. J Physiol 361: 185-204, 1985
18. Elliot AC, Smith GL, Eisner DA, Allen DG: Metabolic changes during ischemia and their role in contractile failure in isolated ferret hearts. J Physiol 454: 467-490, 1992
19. Pan B-S, Solaro RJ: Calcium binding properties of troponin C in detergent-skinned heart muscle fibers. J Biol Chem 262: 7839-7849, 1987