A new milrinone analog: Role of binding to A1 adenosine receptor in its positive inotropic effect on isolated guinea pig and rat atria

Journal of Pharmacology and Experimental Therapeutics

Volumn 283, Issue 2, 1997, Pages 541-547

  Floreani, Maura ^a   Borea, Pier Andrea ^b   Gessi, Stefania ^b   Mosti, Luisa ^c   Fossa, Paola ^c   Dorigo, Paola ^a  

^a UNIVERSITY OF PADOVA   (Italy)

^b UNIVERSITY OF FERRARA   (Italy)

^c UNIVERSITY OF GENOA   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

6 ETHYL 5 PROPIONYL 1,2 DIHYDRO 2 OXO 3 PYRIDINE CARBONITRILE; 8 CYCLOPENTYL 1,3 DIPROPYLXANTHINE; ADENOSINE A1 RECEPTOR; ADENOSINE DEAMINASE; ADENOSINE RECEPTOR STIMULATING AGENT; CARBACHOL; CYCLIC AMP; CYCLOHEXYLADENOSINE; DRUG ANALOG; HEART RECEPTOR; ISOPRENALINE; MILRINONE; PHENYLISOPROPYLADENOSINE; PHOSPHODIESTERASE INHIBITOR; PROPRANOLOL; RESERPINE; TYRAMINE; UNCLASSIFIED DRUG;

ADRENERGIC SYSTEM; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG EFFECT; DRUG MECHANISM; DRUG RECEPTOR BINDING; ENZYME INHIBITION; GUINEA PIG; HEART ATRIUM CONTRACTILITY; HEART ATRIUM CONTRACTION; INOTROPISM; ISOLATED HEART; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR AFFINITY;

ANIMALS; CARDIOTONIC AGENTS; DOSE-RESPONSE RELATIONSHIP, DRUG; GUINEA PIGS; MILRINONE; MYOCARDIAL CONTRACTION; PHOSPHODIESTERASE INHIBITORS; PYRIDONES; RATS; RECEPTORS, PURINERGIC P1;

EID: 0030730411     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (43)

1. ALOUSI, A. A. AND FARAH, A. E.: Letter to the editor. Circ. Res. 46: 887-888, 1980.
2. ALOUSI, A. A., FARAH, A. E., LESHER, G. Y. AND OPALKA, C. J., JR.: Cardiotonic activity of amrinone-WIN 40680 (5′-amino-3,4′-bipyridin 6(1H)-one. Circ. Res. 45: 666-677, 1979.
3. AZARI, J. AND HUXTABLE, R. J.: Differential effects of amrinone on contractility and taurine influx in rat and guinea pig hearts. Eur. J. Pharmacol. 67: 347-353, 1980.
4. BELARDINELLI, L. AND ISENBERG, G.: Isolated atrial myocytes: Adenosine and acetylcholine increase potassium conductance. Am. J. Physiol. 244: H734-H737, 1983.
5. BRUNKHORST, D., VON DER LEYEN, H., MEYER, W., NIGBUR, R., SCHMIDT-SCHUMACHER, C. AND SCHOLZ, H.: Relation of positive inotropic and chronotropic effect 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.
6. CARPENEDO, F., FLOREANI, M. AND CARGNELLI, G.: Competitive inhibition of phosphodiesterase activity by amrinone: Its implication in the cardiac effect of the drug. Pharmacol. Res. Commun. 16: 969-977, 1984.
7. 50) of an enzymatic reaction. Biochem. Pharmacol, 22: 3099-3108, 1973.
8. DIXON, M.: The determination of enzyme inhibitor constant. Biochem. J. 55: 170-171, 1953.
9. DORIGO, P., FRACCAROLLO, D., GAION, R. M., SANTOSTASI, G., BOREA, P. A., FLOREANI, M., MOSTI, L. AND MARAGNO, I.: New inotropic agents: Milrinone analogues. Gen. Pharmacol. 28: 781-788, 1997.
10. DORIGO, P., FRACCAROLLO, D., SANTOSTASI, G., MARAGNO, I., FLOREANI, M., BOREA, P. A., MOSTI, L., SANSEBASTIANO, L., FOSSA, P., ORSINI, F., BENBTOLLO, F. AND BOMBIERI, G.: Synthesis and cardiotonic activity of novel pyrimidine derivatives. Crystallographic and quantum chemical studies. J. Med. Chem. 39: 3671-3683, 1996.
11. DORIGO, P., GAION, R. M., BELLUCO, P., BOREA, P. A., GUERRA, L., MOSTI, L., FLOREANI, M. AND CARPENEDO, F.: Antagonism toward endogenous adenosine and inhibition of cGI-PDE in the cardiac effects of amrinone, milrinone and related analogues. Gen. Pharmacol. 23: 535-541, 1992.
12. DORIGO, P., GAION, R. M., BELLUCO, P., FRACCAROLLO, D., MARAGNO, I., BOMBIERI, G., BENETOLLO, F., MOSTI, L. AND ORSINI, F.: A pharmacological, crystallographic, and quantum chemical study of new inotropic agents. J. Med. Chem. 36: 2475-2484, 1993.
13. DORIGO, P., GAION, R. M., BELLUCO, P., MOSTI, L., BOREA, P. A. AND MARAGNO, I.: An analysis of the mechanisms of the inotropic action of some milrinone analogues in guinea pig isolated atria. Br. J. Pharmacol. 104: 867-872, 1991.
14. DORIGO, P., GAION, R. M. AND MARAGNO, I.: Involvement of purine compounds in the inotropic action of milrinone. Cardiovasc. Drugs Ther. 4: 509-514, 1990.
15. DORIGO, P. AND MARAGNO, I.: Interaction of amrinone with endogenous adenosine in guinea pig atria. Br. J. Pharmacol. 87: 623-629, 1986.
16. EARL, C. Q., LINDEN, J. AND WEGLICKI, W. B.: Biochemical mechanisms for the inotropic effect of the cardiotonic drug milrinone. J. Cardiovasc. Pharmac. 8: 864-872, 1986.
17. ENDOH, M.: Correlation of cyclic AMP and cyclic GMP levels with changes in contractile force of dog ventricular myocardium during cholinergic antagonism of positive actions of histamine, glucagon, theophillin and papaverine. Jpn. J. Pharmacol. 29: 855-864, 1979.
18. ENDOH, M., YAMASHITA, S. AND TAIRA, N.: Positive inotropic effect of amrinone in relation to cyclic nucleotide metabolism in the canine ventricular muscle. J. Pharmacol. Exp. Ther. 221: 775-783, 1982.
19. ENDOH, M., YANAGISAWA, T., TAIRA, N. AND BLINKS, J. R.: Effects of new inotropic agents on cyclic nucleotide metabolism and calcium transients in canine ventricular muscle. Circulation 73: (suppl.III): 117-133, 1986.
20. FARAH, A. E. AND ALOUSI, A. A.: New cardiotonic agents: A search for digitalis substitute. Life Sci. 22: 1139-1148, 1978.
21. FLOREANI, M., FORLIN, A., PANDOLFO, L., PETRONE, M. AND BELLIN, S.: Mechanisms of plumbagin action on guinea pig isolated atria. J. Pharmacol. Exp. Ther. 278: 763-770, 1996.
22. HONERJAEGER, P., SCHAEFER-KORTING, M. AND REITER, M.: Involvement of cyclic AMP in the direct inotropic action of amrinone: Biochemical and functionl evidence. Naunyn Schmiedeberg's Arch. Pharmacol. 318: 112-120, 1981.
23. 2+ uptake by cardiac membrane vesicles. J. Biol. Chem. 252: 3315-3323, 1977.
24. KENAKIN, T. P. AND SCOTT, D. L.: A method to assess concomitant cardiac phosphodiesterase inhibition and positive inotropy. J. Cardiovasc. Pharmacol. 10: 658-666, 1987.
25. KOBYLARZ, D. C., STEFFEN, R. P., WEISHAAR, R. E. AND EVANS, D. B.: Relationship between inhibition of ventricular peak III phosphodiesterase and the in vivo cardiotonic effect of CI-914 in several species. Pharmacologist 27: 603-609, 1985.
26. LATHERS, C. M. AND ROBERTS, J.: Digitalis cardiotoxicity revisited. Life Sci. 27: 1713-1733, 1980.
27. LINEWEAVER, H. AND BURK, D.: The determination of enzyme dissociation constants. J. Amer. Chem. Soc. 56: 658-666, 1934.
28. LOWRY, O. H., ROSEBROUGH, N. J., FARR, A. L. AND RANDALL, R. J.: Protein measurement with the Folin phenol reagent. J. Biol. Chem. 193: 265-275, 1951.
29. LUBBE, W. F., PODZUWETT, T. AND OPIE, L. H.: Potential arrhythmogenic role of cyclic monophosphate (AMP) and cytosolic calcium overload: Implications for prophylactic effects of beta-blockers in myocardial infarction and proar-rhythmic effects of phosphodiesterase inhibitors. J. Am. Cell Cardiol. 19: 1622-1655, 1992.
30. MASON, D. T., ZELIS, R., LEE, G., HUGHES, J. L., SPANN, J. F. AND AMSTERDAM, E. A.: Current concepts and treatment of digitalis toxicity. Am. J. Cardiol. 27: 546-559, 1971.
31. MILLER, R. R., PALOMO, A. R., BRANDON, T. A., HARTLEY, C. J. AND QUINONES, M. A.: Combined vasodilator and inotropic therapy of heart failure: Experimental and clinical concepts. Am. Heart J. 102: 500-508, 1981.
32. MUNSON, P. J. AND RODBARD, D.: Ligand: A versatile computerized approach for the characterization of ligand binding systems. Anal. Biochem. 107: 220-239, 1980.
33. NEWMAN, W. H., GROSSMAN, S. J., FRANKIS, M. B. AND WEBB, J. G.: Increased myocardial adenosine release in heart failure. J. Mol. Cell Cardiol. 16: 577-580, 1984.
34. NICHOLSON, C. D., CHALLISS, R. A. J. AND SHAHID, M.: Differential modulation of tissue function and therapeutic potential of selective inhibitors of cyclic nucleotide phosphodiesterase isoenzymes. Trends Pharmacol. Sci. 12: 19-27, 1991.
35. PACKER, M.: End of the oldest controversy in medicine. Are we ready to conclude the debate on digitalis? N. Eng. J. Med. 336: 575-576, 1997.
36. 1. Mol. Pharmacol. 33: 441-448, 1988.
37. SILVER, P. J., HAMEL, L. T., PERRONE, M. K., BENTLEY, R. G., BUSHOVER, C. R. AND EVANS, D. B.: Differential pharmacological sensitivity of cyclic nucleotide phosphodiesterase isozymes isolated from cardiac muscle, arterial and airway smooth muscle. Eur. J. Pharmacol. 150: 85-90, 1988.
38. SLAUGHTER, R. S., SUTKO, J. L. AND REEVES, J. P.: Equilibrium calcium-calcium exchange in cardiac sarcolemmal vesicles. J. Biol. Chem. 258: 3183-3190, 1983.
39. TAYLOR, S. H., SILKE, B. AND NELSON, G. J. C.: Principles of treatment of left ventricular failure. Eur. Heart J. 3: (suppl.D), 19-43, 1982.
40. THOMPSON, W. J., BROOKER, G. AND APPLEMAN, M. M.: Assay of cyclic nucleotide phosphodiesterase with radioactive substrates. Meth. Enzymol. 38: 205-214, 1974.
41. WARD, A., BRODGEN, R. N., HEEL, R. C., SPEIGHT, T. M. AND AVERY, G. S.: Amrinone: A preliminary review of its pharmacological properties and therapeutic use. Drugs 26: 468-502, 1983.
42. WEISHAAR, R. E., BURROWS, S. D., KOBYLARZ, D. C., QUADE, M. M. AND EVANS, D. B.: Multiple molecular forms of cyclic nucleotide phosphodiesterase in cardiac and smooth muscle and in platelets. Biochem. Pharmacol. 35: 787-800, 1986.
43. WEISHAAR, R. E., KOBYLARZ-SINGER, D. L., STEFFEN, R. P. AND KAPLAN, A. R.: Subclasses of cyclic AMP specific phosphodiesterase in left ventricular muscle and their involvement in regulating myocardial contractility. Circ. Res. 61: 539-547, 1987.