Mechanism underlying the strong positive inotropic effects of LND-623: Specific inhibition of Na, K-ATPase isoforms and exclusion of cellular sites of contractile control

Cardiovascular Drugs and Therapy

Volumn 12, Issue 6, 1998, Pages 585-594

  Maixent, Jean Michel ^a   Lelièvre, Lionel ^b   Berrebi Bertrand, Isabelle ^a,c  

^a AIX MARSEILLE UNIVERSITY   (France)

^b UNIVERSITÉ PARIS DESCARTES   (France)

^c SmithKline Beecham   (France)

Author keywords

Aminosteroid; Digitalis; Heart; Human erythrocyte; Inotropy; Rat; Sodium pump

Indexed keywords

14BETA AMINO 5BETA PREGNAN 20BETA OL 3 RHAMNOSIDE; ADENOSINE TRIPHOSPHATASE (POTASSIUM SODIUM); OUABAIN; SODIUM ION;

ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG MECHANISM; ENZYME INHIBITION; ERYTHROCYTE; INOTROPISM; ISOLATED HEART; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; SODIUM TRANSPORT;

ADENYLATE CYCLASE; ANIMALS; CARDIOTONIC AGENTS; DOGS; ERYTHROCYTES; HUMANS; ISOENZYMES; MALE; MANNOSIDES; MEMBRANES; MYOCARDIAL CONTRACTION; MYOFIBRILS; NA(+)-K(+)-EXCHANGING ATPASE; OUABAIN; PHOSPHORIC DIESTER HYDROLASES; PREGNANES; RATS; RATS, WISTAR; SODIUM-CALCIUM EXCHANGER;

EID: 0032450459     PISSN: 09203206     EISSN: None     Source Type: Journal    
DOI: 10.1023/A:1007747623749     Document Type: Article

References (41)

1. 1. Smith TW. Digoxin in heart failure. N Engl J Med 1993;329:51-53.
2. 2. Gheorghiade M. Digoxin therapy in chronic heart failure. Cardiovasc Drugs Ther 1997;11;279-283.
3. 3. Jarreau FX, Koening JJ, Fenard S. A new inotropic aminosteroid: LND623. Eur Heart J 1984;5:309-311.
4. 4. Adamantidis NM, Honoré ER, Dupuis BM. Electrical and mechanical effects of new aminosteroids on guinea pig isolated ventricular muscle. Br J Pharmacol 1988;95: 1063-1074.
5. 5. Maixent JM, Berrebi-Bertrand I, Lelièvre LG. Inhibition of cardiac Na, K-ATPase isozymes by LND-623. Biochem Pharmacol 1991;42:S223-S224.
6. 6. Maixent J M, Berrebi-Bertrand I, Lelièvre L G, Fénard S. Efficacy and safety of the novel Na, K-ATPase inhibitor 20β R 14β-amino, 3β rhamnosyl, 5β pregnan, 20β-ol) in a model of heart failure. Arzn Forsch Drug Res 1092;42:1301-1305.
7. 7. Schönfeld W, Weiland J, Repke KRH. Biochemical basis for the targeted synthesis of cardiac glycosides with selective action. In: Erdmann E, Greef, K, Skou JS, eds. Cardiac Glycosides (1785-1985). Darmstadt:, Steinkopff Verlag 1986:127-134.
8. 8. Kawamoto RM, Pong SF, Simmons M, Chang YC, Maixent JM. Characterization of [3H] LND-796 binding to renal and neural and cardiac membrane fractions. Pharm Pharmacol Lett 1995;4:150-153.
9. 9. Maixent JM, Gerbi A, Barbey O, Fénard S, Kawamoto RM, Baggioni A. Relation of plasma concentrations to positive inotropic effect of intravenous administration of cordil in dogs. Pharm Pharmacol Lett 1995;2:1-4.
10. 10. Reiter M. Calcium mobilization and cardiac inotropic mechanisms. Pharmacol Rev 1988;40:189-217.
11. 11. Erdmann E, Philip G, Scholz H. Cardiac glycoside receptor Na,K-ATPase activity and force of contraction in rat heart. Biochem Pharmacol 1980;29:3219-3229.
12. 12. Adams RJ, Schwartz A, Grupp G, et al. High affinity binding site and low-dose inotropic effect in rat myocardium. Nature 1982;296:167-169.
13. 13. Lelièvre LG, Maixent JM, Lorente P, Mouas C, Charlemagne D, Swynghedauw B. Prolonged responsiveness to ouabain in hypertrophied rat heart: Physiological and biochemical evidence. Am J Physiol 1986;250:H923-H931.
14. 14. Sweadner KJ. Isoenzymes of the Na,K-ATPase. Biochim Biophys Acta 1989;145:185-220.
15. 15. Grupp I, Im WB, Lee CO, Lee SW. Relation of sodium pump inhibition to positive inotropy at low concentrations of ouabain in rat heart muscle. J Physiol 1985;360:149-160.
16. 16. Sweadner KJ. Multiple digitalis receptors, a molecular perspective. Trends Cardiovasc Med 1993;3:2-6.
17. 17. De Pover A, Grupp G, Schwartz A, Grupp IL. Coupling of contraction through effects on Na,K-ATPase: Changes in Na,K-ATPase isoforms in heart disease? Heart Failure 1990;1:201-258.
18. 18. Maixent JM, Charlemagne D, De La Chapelle B, Lelièvre LG. Two Na,K-ATPase isoenzymes in canine cardiac myocytes: Molecular basis of inotropic and toxic effects of digitalis. J Biol Chem 1987;262:6842-6848.
19. 2+ -free perfusion in rat heart reveals a Na, K-ATPase form highly sensitive to ouabain. Nature 1982;300:535-537.
20. 20. Janicot M, Desbuquois B. Fate of injected (125-I) cholera toxin taken up by rat liver in vivo: Generation of the active A1 peptide in the endosomal compartment. Eur J Biochem 1987;163:433-442.
21. 21. Garay RP, Diez J, Nazaret C, Dagher G, Abitbol JP. The interaction of canrenone with the Na,K-pump in human red blood cells. Naunyn Schiedebergs Arch Pharmacol 1985;329:311-319.
22. 22. Chamberlain BK, Volpe P, Fleicher S. Inhibition of calcium induced calcium release from purified cardiac sarcoplasmic reticulum vesicles. J Biol Chem 1984;259:7540-7546.
23. 2+ binding and ATPase activity of dog cardiac myofibrils by AR-L115BS, a novel cardiotonic agent. Circ Res 1982;51:290-294.
24. 24. Pitts BJR. Stoiechiometry of sodium/calcium exchange in cardiac sarcolemma vesicles. J Biol Chem 1979;254: 6232-6236.
25. 25. Salomon Y, Londos C, Rodbell M. A highly sensitive adenylate cyclase assay. Anal Biochem 1974;58:541-546.
26. 26. Konas N, Lugnier C, Le Bec A, Serradeil-Le Gal C, Barthelemy G, Stoclet JC. Differential sensitivity to cardiotonic dings of cAMP phosphodiesterases isolated from canine ventricular and sinoatrial-enriched tissues. J Cardiovasc Pharmacol 1989;14:213:220.
27. 27. Khananshili D, Weil-Maslansky E. The cardiac Na/Ca exchanger: Relative rates of calcium and sodium movements and their modulation by protonation-deprotonation of the carrier. Biochemistry 1994;33:312-319.
28. 2+ -release channels: A possible role in cardiac inotropy. Br J Pharmacol 1993;108:1043-1050.
29. 29. Weingardt R, Marban E, Tsien RW. Is digitalis inotropy associated with enhanced slow inward calcium current? Nature 1978;273:389-391.
30. 30. Marban E, Tsien RW. Enhancement of calcium current during digitalis inotropy in mammalian heart: Positive feedback regulation by intracellular calcium? J Physiol 1982; 329:580-585.
31. 31. Finkel MS, Romeo RC, Hartsell TL, Oddis CV. BAYK8644 is a negative inotropic in the presence of arachidonic acid but not eicopentaenoic acid. J Cardiovasc Pharmacol 1992; 20:563-571.
32. 32. Hallaq H, Smith TW, Leaf A. Modulation of dihydropyridine-sensitive calcium channels in heart cells by fish oil fatty acids. Proc Natl Acad Sci USA 1992;89:1760-1704.
33. 33. Brown L. Positive inotropic and vasoconstrictor responses to 14 β-aminopregnane derivates in isolated tissues from guinea pig. Clin Exp Pharm Physiol. 1990;17:589-594.
34. 34. Shamraj OI, Grupp IL, Grupp G, et al. Characterization of Na/K-ATPase, its isoforms, and the inotropic response to ouabain in isolated failing human hearts. Cardiovasc Res 1993;27:2229-2237.
35. 35. Zahler R, Gimore-Hebert M, Baldwin JC, Franco K, Benz EJ, Jr. Expression of isoforms of the Na,K-ATPase in human heart. Biochim Biophys Acta 1993;1149:189-194.
36. 36. Barbey O, Gerbi A, Robert K, Mayol V, Pierre S, Paganelli, Maixent JM. Immunological identification of Na,K-ATPase alpha subunit isoforms in nonfailing and failing myocardium. Ann NY Acad Sci 1997;834:658-660.
37. 37. Askew GR, Lingrel JB, Grupp IL, Grupp G. Direct correlation of Na,K-ATPase-isoform abundance and myocardial contractility in mouse heart. In: E. Bamberg, W Schoner, eds. The Sodium Pump: Structure, Mechanism, Hormonal Control and its Role in Disease. Darmstadt: Steinkopff; New York: Springer, 1994:718-721.
38. 38. Maixent JM, Gerbi A, Berrebi-Bertrand I, Correa P, Genain G, Baggioni A. Cordil reversibly inhibits the Na, K-ATPase from outside of the cell membrane. Role of K-dependent dephosphorylation. J Recept Res 1993;13:1083-1092.
39. 39. Maixent JM, Fénard S, Kawamoto RM. Tissue localization of active Na,K-ATPase isoenzymes by determination of their profile of inhibition with ouabain, digoxin, digitoxigenin and LND 796, a new aminosteroid cardiotonic. J Recept Res 1991;11:687-698.
40. 40. Scholtysik K, Salzmann R, Berthold R, Herzig JN, Quast U, Markstein R. DPI 201-106, a novel cardioactive agent. Combination of cAMP-independent positive inotropic, negative chronotropic, action potential prolonging and coronary dilatory properties. Naunyn Schiedebergs Arch Pharmacol 1988;329:316-325.
41. 41. Malloy KJ, David BC, Dhillon DS. LND-796, a potent cardiotonic drug with improved safety vs. digoxin (abstr). Circulation 1989;80:S129.