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Chemical Compound Review

Bucindolol     2-[2-hydroxy-3-[[1-(1H-indol- 3-yl)-2...

Synonyms: Bucindololum, SureCN20138, CHEMBL321582, AG-G-78346, CHEBI:259883, ...
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Disease relevance of Bucindolol


High impact information on Bucindolol

  • However, the Arg-389 homozygotes treated with bucindolol had an age-, sex-, and race-adjusted 38% reduction in mortality (P = 0.03) and 34% reduction in mortality or hospitalization (P = 0.004) vs. placebo [6].
  • Dose-response of chronic beta-blocker treatment in heart failure from either idiopathic dilated or ischemic cardiomyopathy. Bucindolol Investigators [7].
  • There was a dose-related improvement in left ventricular function in bucindolol-treated subjects [7].
  • We investigated the effects of bucindolol, a nonselective, non-ISA beta-blocker with mild-vasodilatory properties, in patients with congestive heart failure from ischemic dilated cardiomyopathy (ISCDC, n = 27) and compared the results with those in subjects with heart failure from idiopathic dilated cardiomyopathy (IDC, n = 22) [8].
  • Patients were randomized in a double-blind fashion to receive 12 weeks' treatment with either bucindolol or placebo, with randomization stratified for IDC or ISCDC [8].

Chemical compound and disease context of Bucindolol


Biological context of Bucindolol

  • At a matched paced heart rate of 98 +/- 15 min-1, the time constant of left ventricular isovolumic relaxation was significantly reduced by bucindolol therapy (92 +/- 17 versus 73 +/- 11 msec, p = 0.0013), and the relation of the time constant to end-systolic pressure was shifted downward (p = 0.014) with therapy [1].
  • Thus, in patients with congestive heart failure, chronic beta-adrenergic blockade with bucindolol significantly improves myocardial contractility and minute work, yet it does not do so at the expense of myocardial oxygen consumption [1].
  • Patients treated with bucindolol also had a significant increase in exercise left ventricular ejection fraction (0.26 +/- 0.03 to 0.32 +/- 0.14, p = 0.015) and reduction in questionnaire-measured symptoms (p = 0.007) and New York Heart Association functional class (p less than 0.001) [12].
  • The property of gaunine nucleotide-modulatable binding for carvedilol and structurally related bucindolol correlates with their ability to directly down-regulate beta 1-like receptors present in cultured chick myocytes, and with a lack of reversal of down-regulation of cardiac beta-receptors in patients with heart failure [13].
  • Standing diastolic blood pressure was significantly reduced by bucindolol 200 and 400 mg [14].

Anatomical context of Bucindolol


Associations of Bucindolol with other chemical compounds


Gene context of Bucindolol


Analytical, diagnostic and therapeutic context of Bucindolol


  1. Effect of beta-adrenergic blockade on myocardial function and energetics in congestive heart failure. Improvements in hemodynamic, contractile, and diastolic performance with bucindolol. Eichhorn, E.J., Bedotto, J.B., Malloy, C.R., Hatfield, B.A., Deitchman, D., Brown, M., Willard, J.E., Grayburn, P.A. Circulation (1990) [Pubmed]
  2. Efficacy of bucindolol in systemic hypertension. Kimura, S., DeQuattro, V., Edmiston, W.A., Loo, R., Thien, S., Rigonan, K., Deitchman, D., Foti, A. Am. J. Cardiol. (1987) [Pubmed]
  3. The incomplete bucindolol evaluation in acute myocardial infarction Trial (BEAT). Torp-Pedersen, C., Køber, L., Ball, S., Hall, A., Brendorp, B., Ottesen, M., Berning, J., Jensen, G., Hampton, J., Zilles, P., Eberle, S., Carlsen, J. Eur. J. Heart Fail. (2002) [Pubmed]
  4. A comparison of single doses of bucindolol and oxprenolol in hypertensive patients. Webster, J., Petrie, J.C., Robb, O.J., Jamieson, M., Verschueren, J. British journal of clinical pharmacology. (1985) [Pubmed]
  5. Bucindolol, a beta-adrenoceptor blocker with vasodilatory action: its effect in systemic hypertension. Rotmensch, H.H., Rocci, M.L., Vlasses, P.H., Swanson, B.N., Fedder, I.L., Soyka, L., Ferguson, R.K. Am. J. Cardiol. (1984) [Pubmed]
  6. A polymorphism within a conserved beta(1)-adrenergic receptor motif alters cardiac function and beta-blocker response in human heart failure. Liggett, S.B., Mialet-Perez, J., Thaneemit-Chen, S., Weber, S.A., Greene, S.M., Hodne, D., Nelson, B., Morrison, J., Domanski, M.J., Wagoner, L.E., Abraham, W.T., Anderson, J.L., Carlquist, J.F., Krause-Steinrauf, H.J., Lazzeroni, L.C., Port, J.D., Lavori, P.W., Bristow, M.R. Proc. Natl. Acad. Sci. U.S.A. (2006) [Pubmed]
  7. Dose-response of chronic beta-blocker treatment in heart failure from either idiopathic dilated or ischemic cardiomyopathy. Bucindolol Investigators. Bristow, M.R., O'Connell, J.B., Gilbert, E.M., French, W.J., Leatherman, G., Kantrowitz, N.E., Orie, J., Smucker, M.L., Marshall, G., Kelly, P. Circulation (1994) [Pubmed]
  8. Beta-blockade with bucindolol in heart failure caused by ischemic versus idiopathic dilated cardiomyopathy. Woodley, S.L., Gilbert, E.M., Anderson, J.L., O'Connell, J.B., Deitchman, D., Yanowitz, F.G., Mealey, P.C., Volkman, K., Renlund, D.G., Menlove, R. Circulation (1991) [Pubmed]
  9. Hemodynamic and energetic comparison of bucindolol and metoprolol for the treatment of congestive heart failure. Heesch, C.M., Marcoux, L., Hatfield, B., Eichhorn, E.J. Am. J. Cardiol. (1995) [Pubmed]
  10. Effects of bucindolol on neurohormonal activation in congestive heart failure. Eichhorn, E.J., McGhie, A.L., Bedotto, J.B., Corbett, J.R., Malloy, C.R., Hatfield, B.A., Deitchman, D., Willard, J.E., Grayburn, P.A. Am. J. Cardiol. (1991) [Pubmed]
  11. Evaluation of intrinsic sympathomimetic activity of bucindolol and carvedilol in rat heart. Willette, R.N., Mitchell, M.P., Ohlstein, E.H., Lukas, M.A., Ruffolo, R.R. Pharmacology (1998) [Pubmed]
  12. Long-term beta-blocker vasodilator therapy improves cardiac function in idiopathic dilated cardiomyopathy: a double-blind, randomized study of bucindolol versus placebo. Gilbert, E.M., Anderson, J.L., Deitchman, D., Yanowitz, F.G., O'Connell, J.B., Renlund, D.G., Bartholomew, M., Mealey, P.C., Larrabee, P., Bristow, M.R. Am. J. Med. (1990) [Pubmed]
  13. Cardiac adrenergic receptor effects of carvedilol. Yoshikawa, T., Port, J.D., Asano, K., Chidiak, P., Bouvier, M., Dutcher, D., Roden, R.L., Minobe, W., Tremmel, K.D., Bristow, M.R. Eur. Heart J. (1996) [Pubmed]
  14. Comparison of the haemodynamic effects of bucindolol, propranolol and pindolol in healthy volunteers. O'Connor, P.C., Finch, M.J., Harron, D.W., Meredith, P.A., McDevitt, D.G., Shanks, R.G. British journal of clinical pharmacology. (1985) [Pubmed]
  15. Bucindolol exerts agonistic activity on the propranolol-insensitive state of beta1-adrenoceptors in human myocardium. Bundkirchen, A., Brixius, K., Bölck, B., Schwinger, R.H. J. Pharmacol. Exp. Ther. (2002) [Pubmed]
  16. Pharmacology of bucindolol in isolated canine vascular smooth muscle. Rimele, T.J., Aarhus, L.L., Lorenz, R.R., Rooke, T.W., Vanhoutte, P.M. J. Pharmacol. Exp. Ther. (1984) [Pubmed]
  17. Different intrinsic activities of bucindolol, carvedilol and metoprolol in human failing myocardium. Maack, C., Cremers, B., Flesch, M., Höper, A., Südkamp, M., Böhm, M. Br. J. Pharmacol. (2000) [Pubmed]
  18. In vitro and in vivo characterization of intrinsic sympathomimetic activity in normal and heart failure rats. Willette, R.N., Aiyar, N., Yue, T.L., Mitchell, M.P., Disa, J., Storer, B.L., Naselsky, D.P., Stadel, J.M., Ohlstein, E.H., Ruffolo, R.R. J. Pharmacol. Exp. Ther. (1999) [Pubmed]
  19. Vasodilating beta-adrenoceptor blocking drugs do not redistribute myocardial flow during acute coronary ligation in dogs. Berdeaux, A., Bonhenry, C., Giudicelli, J.F. Eur. J. Pharmacol. (1985) [Pubmed]
  20. Partial agonist activity of bucindolol is dependent on the activation state of the human beta1-adrenergic receptor. Maack, C., Böhm, M., Vlaskin, L., Dabew, E., Lorenz, K., Schäfers, H.J., Lohse, M.J., Engelhardt, S. Circulation (2003) [Pubmed]
  21. Interaction of the beta adrenergic receptor antagonist bucindolol with serotonergic receptors. Watts, S.W., Fink, G.D., Silver, P.J., Cushing, D.J. J. Cardiovasc. Pharmacol. (2000) [Pubmed]
  22. Hemodynamic properties of bucindolol, a beta-adrenoreceptor blocking drug with vasodilator activity. Bett, N., Dryburgh, L., Boyle, C., Hawley, C. Am. J. Cardiol. (1986) [Pubmed]
  23. Bucindolol, a beta blocker, decreased ventricular fibrillation and maintained mechanical function in a pig model of acute myocardial ischemia. Muller, C.A., Opie, L.H., Pineda, C.A., Peisach, M. Cardiovascular drugs and therapy / sponsored by the International Society of Cardiovascular Pharmacotherapy. (1992) [Pubmed]
  24. Importance of a history of hypertension for the prognosis after acute myocardial infarction--for the Bucindolol Evaluation in Acute myocardial infarction Trial (BEAT) study group. Ali, I., Akman, D., Bruun, N.E., Køber, L., Brendorp, B., Ottesen, M., Møller, J., Torp-Pedersen, C. Clinical cardiology. (2004) [Pubmed]
  25. Studies on the vasodilator actions of bucindolol in the rat. Marwood, J.F., Stokes, G.S. Clin. Exp. Pharmacol. Physiol. (1986) [Pubmed]
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