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Chemical Compound Review

Bystolic     1-(6-fluorochroman-2-yl)-2- [[2-(6...

Synonyms: Nebilong, Nebipill, Lobivon, Nebilet, Nebivolol, ...
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Disease relevance of Nebivolol


High impact information on Nebivolol

  • Nebivolol and its 4-keto derivative increase nitric oxide in endothelial cells by reducing its oxidative inactivation [5].
  • OBJECTIVES: The objective of the present study was to elucidate the vasodilator mechanisms of nebivolol, a high selective beta(1)-receptor antagonist with antioxidant properties [5].
  • The preincubation of BAECs with blocking anti-LOX-1 monoclonal antibody (LOX-1 mAb) significantly counteracted the effect of ox-LDL on stimulated generation of NO (p < 0.001), but the effect was significantly lower than that of nebivolol and its 4-keto derivative alone (p < 0.01) [5].
  • Despite a decrease in heart rate with nebivolol, there was a slight decrease in left ventricular end-diastolic volume (p = NS) [6].
  • Exercise time, invasive hemodynamic data (12- and 24-h monitoring) and variables of left ventricular function were examined at baseline and after 3 months of orally administered nebivolol (1 to 5 mg/day, n = 11) or placebo (n = 13) [6].

Chemical compound and disease context of Nebivolol

  • OBJECTIVE : To investigate whether chronic selective beta1-blockade with nebivolol could prevent endothelial dysfunction in salt-induced hypertension, and to compare it with atenolol [7].
  • METHODS: One day after induction of anti-thy1 glomerulonephritis, rats were given increasing doses of the beta-blockers metoprolol or nebivolol (0.1-fold, one-fold, 10-fold and 20-fold of the known blood pressure dose) until day 6 and the 20-fold dose until day 12 [8].
  • We provided evidence that nebivolol, given as monotherapy or in combination with low dose of hydrochlorothiazide, is effective in reducing clinic and 24-h ambulatory blood pressure in patients with ambulatory hypertension [9].
  • After a washout period of 8 weeks, 51 patients with mild to moderate essential hypertension were randomized to double-blind treatment with either nebivolol 5 mg once a day (n = 26) or nifedipine sustained-release 20 mg bid (n = 25) over a period of 12 weeks [10].
  • METHODS: In a double-blind, randomized, parallel group study 314 patients with hypertension were treated for 12 weeks with 5 mg of nebivolol or 50 mg of losartan once daily [11].

Biological context of Nebivolol


Anatomical context of Nebivolol


Associations of Nebivolol with other chemical compounds


Gene context of Nebivolol


Analytical, diagnostic and therapeutic context of Nebivolol


  1. Effects of nebivolol in elderly heart failure patients with or without systolic left ventricular dysfunction: results of the SENIORS echocardiographic substudy. Ghio, S., Magrini, G., Serio, A., Klersy, C., Fucilli, A., Ronaszèki, A., Karpati, P., Mordenti, G., Capriati, A., Poole-Wilson, P.A., Tavazzi, L. Eur. Heart J. (2006) [Pubmed]
  2. Nebivolol in hypertension and chronic heart failure: a viewpoint by alberto zanchetti. Zanchetti, A. Drugs (2006) [Pubmed]
  3. Cardiovascular effects of nebivolol in spontaneously hypertensive rats persist after treatment withdrawal. Guerrero, E.I., Ardanaz, N., Sevilla, M.A., Arévalo, M.A., Montero, M.J. J. Hypertens. (2006) [Pubmed]
  4. Nebivolol improves coronary flow reserve in hypertensive patients without coronary heart disease. Galderisi, M., Cicala, S., D'Errico, A., de Divitiis, O., de Simone, G. J. Hypertens. (2004) [Pubmed]
  5. Nebivolol and its 4-keto derivative increase nitric oxide in endothelial cells by reducing its oxidative inactivation. Cominacini, L., Fratta Pasini, A., Garbin, U., Nava, C., Davoli, A., Criscuoli, M., Crea, A., Sawamura, T., Lo Cascio, V. J. Am. Coll. Cardiol. (2003) [Pubmed]
  6. Long-term (3-month) effects of a new beta-blocker (nebivolol) on cardiac performance in dilated cardiomyopathy. Wisenbaugh, T., Katz, I., Davis, J., Essop, R., Skoularigis, J., Middlemost, S., Röthlisberger, C., Skudicky, D., Sareli, P. J. Am. Coll. Cardiol. (1993) [Pubmed]
  7. Nitric-oxide-mediated relaxations in salt-induced hypertension: effect of chronic beta1 -selective receptor blockade. Cosentino, F., Bonetti, S., Rehorik, R., Eto, M., Werner-Felmayer, G., Volpe, M., Lüscher, T.F. J. Hypertens. (2002) [Pubmed]
  8. Angiotensin-converting enzyme inhibition but not beta-adrenergic blockade limits transforming growth factor-beta overexpression in acute normotensive anti-thy1 glomerulonephritis. Peters, H., Rückert, M., Gaedeke, J., Liefeldt, L., Ketteler, M., Sharma, A.M., Neumayer, H.H. J. Hypertens. (2003) [Pubmed]
  9. Treatment of ambulatory hypertensives with nebivolol or hydrochlorothiazide alone and in combination. A randomized, double-blind, placebo-controlled, factorial-design trial. Lacourcière, Y., Lefebvre, J., Poirier, L., Archambault, F., Arnott, W. Am. J. Hypertens. (1994) [Pubmed]
  10. Comparative effects of a new cardioselective beta-blocker nebivolol and nifedipine sustained-release on 24-hour ambulatory blood pressure and plasma lipoproteins. Lacourcière, Y., Poirier, L., Lefebvre, J., Provencher, P., Arnott, W. Journal of clinical pharmacology. (1992) [Pubmed]
  11. Quality of life and antihypertensive effect with nebivolol and losartan. Van Bortel, L.M., Bulpitt, C.J., Fici, F. Am. J. Hypertens. (2005) [Pubmed]
  12. Beta-blockade with nebivolol enhances the acetylcholine-induced cutaneous vasodilation. Kubli, S., Feihl, F., Waeber, B. Clin. Pharmacol. Ther. (2001) [Pubmed]
  13. The receptor binding profile of the new antihypertensive agent nebivolol and its stereoisomers compared with various beta-adrenergic blockers. Pauwels, P.J., Gommeren, W., Van Lommen, G., Janssen, P.A., Leysen, J.E. Mol. Pharmacol. (1988) [Pubmed]
  14. Nebivolol decreases oxidative stress in essential hypertensive patients and increases nitric oxide by reducing its oxidative inactivation. Fratta Pasini, A., Garbin, U., Nava, M.C., Stranieri, C., Davoli, A., Sawamura, T., Lo Cascio, V., Cominacini, L. J. Hypertens. (2005) [Pubmed]
  15. Effects of vasodilatory beta-adrenoceptor antagonists on endothelium-derived nitric oxide release in rat kidney. Kakoki, M., Hirata, Y., Hayakawa, H., Nishimatsu, H., Suzuki, Y., Nagata, D., Suzuki, E., Kikuchi, K., Nagano, T., Omata, M. Hypertension (1999) [Pubmed]
  16. Effects of nebivolol on proliferation and apoptosis of human coronary artery smooth muscle and endothelial cells. Brehm, B.R., Wolf, S.C., Bertsch, D., Klaussner, M., Wesselborg, S., Schüler, S., Schulze-Osthoff, K. Cardiovasc. Res. (2001) [Pubmed]
  17. Characterization of beta(1)-selectivity, adrenoceptor-G(s)-protein interaction and inverse agonism of nebivolol in human myocardium. Maack, C., Tyroller, S., Schnabel, P., Cremers, B., Dabew, E., Südkamp, M., Böhm, M. Br. J. Pharmacol. (2001) [Pubmed]
  18. Comparative effects of nebivolol and metoprolol on oxidative stress, insulin resistance, plasma adiponectin and soluble P-selectin levels in hypertensive patients. Celik, T., Iyisoy, A., Kursaklioglu, H., Kardesoglu, E., Kilic, S., Turhan, H., Yilmaz, M.I., Ozcan, O., Yaman, H., Isik, E., Fici, F. J. Hypertens. (2006) [Pubmed]
  19. Nebivolol in the management of essential hypertension: a review. McNeely, W., Goa, K.L. Drugs (1999) [Pubmed]
  20. Effects of nebivolol, atenolol and propranolol on in vivo cardiovascular and metabolic responses to isoproterenol in dogs. Bowden, C.R., Marchione, C.S. J. Pharmacol. Exp. Ther. (1989) [Pubmed]
  21. Nebivolol induces calcium-independent signaling in endothelial cells by a possible beta-adrenergic pathway. Gosgnach, W., Boixel, C., Névo, N., Poiraud, T., Michel, J.B. J. Cardiovasc. Pharmacol. (2001) [Pubmed]
  22. Endothelial beta3-adrenoreceptors mediate nitric oxide-dependent vasorelaxation of coronary microvessels in response to the third-generation beta-blocker nebivolol. Dessy, C., Saliez, J., Ghisdal, P., Daneau, G., Lobysheva, I.I., Frérart, F., Belge, C., Jnaoui, K., Noirhomme, P., Feron, O., Balligand, J.L. Circulation (2005) [Pubmed]
  23. Nebivolol Inhibits Superoxide Formation by NADPH Oxidase and Endothelial Dysfunction in Angiotensin II-Treated Rats. Oelze, M., Daiber, A., Brandes, R.P., Hortmann, M., Wenzel, P., Hink, U., Schulz, E., Mollnau, H., von Sandersleben, A., Kleschyov, A.L., Mülsch, A., Li, H., Förstermann, U., Münzel, T. Hypertension (2006) [Pubmed]
  24. Location of the hydroxyl functions in hydroxylated metabolites of nebivolol in different animal species and human subjects as determined by on-line high-performance liquid chromatography-diode-array detection. Hendrickx, J., Bockx, M., Zwijsen, C., Borgmans, C., Mannens, G., Meuldermans, W., Heykants, J. Journal of chromatography. A. (1996) [Pubmed]
  25. The role of the new beta-blockers in treating cardiovascular disease. Weber, M.A. Am. J. Hypertens. (2005) [Pubmed]
  26. Effect of forced titration of nebivolol on response rate in obese hypertensive patients. Pischon, T., Sharma, A.M., Mansmann, U., Agrawal, R. Am. J. Hypertens. (2003) [Pubmed]
  27. Beta 1-adrenoceptor selectivity of nebivolol and bisoprolol. A comparison of [3H]CGP 12.177 and [125I]iodocyanopindolol binding studies. Bundkirchen, A., Brixius, K., Bölck, B., Nguyen, Q., Schwinger, R.H. Eur. J. Pharmacol. (2003) [Pubmed]
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