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Chemical Compound Review

PENBUTOLOL(-)     1-(2-cyclopentylphenoxy)-3- (tert...

Synonyms: SureCN49358, BSPBio_000966, SPBio_002903, BPBio1_001064, AC1L1ITB, ...
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Disease relevance of penbutolol

  • The effects of penbutolol 20-30 mg twice daily and of metoprolol 50-150 mg three times daily were studied in five and nine patients, respectively, with moderate hypertension [1].
  • Haemodynamic dose-response effects of i.v. penbutolol in angina pectoris [2].
  • 3 Penbutolol proved to be a non-cardioselective beta-adrenoceptor blocking drug, antagonizing exercise-induced tachycardia, reducing exercise-induced increase in PEFR and decreasing PRA [3].
  • The lack of significant bradycardia and the low incidence of other troublesome adverse effects are potential advantages during antihypertensive therapy with penbutolol [4].
  • In the Ames test penbutolol showed significant toxicity above 500 micrograms/plate [5].

Psychiatry related information on penbutolol


High impact information on penbutolol


Chemical compound and disease context of penbutolol


Biological context of penbutolol

  • All derivatives are capable of displacing [3H]BTX-B from its specific binding site, penbutolol displaying the highest affinity [17].
  • The mean systolic pressures of these patients decreased by 21 mm Hg and their mean diastolic pressure decreased by 11 mm Hg during treatment with penbutolol [18].
  • Decline in mean heart rate after 6 weeks of penbutolol therapy significantly exceeded placebo only at 40 mg/day (7.2 vs 2.5 beats/min, p less than 0.05) [4].
  • Decrease in penbutolol protein binding as a consequence of treatment with some alkylating agents [19].
  • Additionally, no significant incorporation of [3H]thymidine into the DNA in the UDS test or formation of DNA-strand breaks in the alkaline elution assay was detected in the non-toxic concentration range of penbutolol with or without metabolic activation [5].

Anatomical context of penbutolol

  • 5. The beta-adrenoceptor blocking agent penbutolol was shown to possess adrenergic neurone blocking activity in the isolated vas deferens of the rat [20].
  • Penbutolol resulted in a linear decrease in heart rate (maximum delta HR - 4 beats/min; P less than 0.01); there was a small increase in pulmonary artery occluded pressure which reached its maximum at the lower doses (maximum delta PAOP + 1 mm Hg; P less than 0.01) [2].
  • The haemodynamic dose-response effects of intravenous penbutolol, a newer beta-adrenoceptor antagonist with intrinsic sympathomimetic activity but without cardioselectivity, were evaluated in 10 patients with angiographically documented coronary artery disease [2].
  • Penbutolol was cytotoxic to human fibroblasts and Chinese hamster V79 cells [21].
  • Beta-adrenoceptor binding of (-) penbutolol and its active metabolite 4-hydroxy-penbutolol to rat reticulocyte membranes was shown in the presence of native human plasma [22].

Associations of penbutolol with other chemical compounds


Gene context of penbutolol

  • The increase in the behavioural deficit induced by 8-OH-DPAT, was likely to have resulted from stimulation of 5-HT1A receptors, since it was impaired by pretreatment with penbutolol, a beta-adrenergic-blocking drug, also known to bind to 5-HT1 receptors [28].
  • The results of the present study demonstrate the absence of genotoxic activity of penbutolol in the 5 strains of Salmonella typhimurium (TA98, TA100, TA1535, TA1537 and TA1538) and in the strain of Escherichia coli WP2 uvrA in the presence or absence of metabolic activation [5].
  • Recently, we found that the beta 1/beta 2 adrenoceptor blocking agent (-)penbutolol prevents behavioral and biochemical actions of the specific serotonin (5-HT)1A agonist (+/-)-8-hydroxy-2-(di-n-propylamino)tetralin [23].
  • Local (-)penbutolol (1 microM) perfusion increased the 5-HT output per se, and also blocked 5-HT release suppression caused by the 5-HT1B receptor agonist CP-93,129 [23].
  • The genotoxic potential of the beta-adrenergic blocker penbutolol was assessed using the Ames and HGPRT tests, unscheduled DNA synthesis (UDS) and alkaline elution assays [5].

Analytical, diagnostic and therapeutic context of penbutolol

  • As is the case with most other beta-blocking drugs, penbutolol has some specific properties (e.g. relatively narrow dose-response range minimising the difficulty of dose titration, moderate intrinsic sympathomimetic activity) which may be used to advantage in certain patients [29].
  • In vivo microdialysis evidence for central serotonin1A and serotonin1B autoreceptor blocking properties of the beta adrenoceptor antagonist (-)penbutolol [23].
  • 5 Comparison of plasma levels and biological activity of penbutolol revealed that after oral administration this drug is transformed into an active metabolite in man [3].
  • Subjects were randomly administered penbutolol, propranolol L.A. and placebo according to a double-blind, three-part cross-over design [6].
  • Determination of penbutolol and its hydroxylated metabolite in biological fluids by reversed-phase high-performance liquid chromatography [30].


  1. Effects of penbutolol and metoprolol on blood pressure, plasma catecholamines and renin activity in hypertensive patients. Hansson, B.G., Dymling, J.F., Manhem, P., Hökfelt, B. Eur. Heart J. (1983) [Pubmed]
  2. Haemodynamic dose-response effects of i.v. penbutolol in angina pectoris. Silke, B., Verma, S.P., Hussain, M., Nelson, G.I., Okoli, R.C., Taylor, S.H. British journal of clinical pharmacology. (1983) [Pubmed]
  3. Comparative beta-adrenoceptor blocking effects and pharmacokinetics of penbutolol and propranolol in man. Giudicelli, J.F., Richer, C., Chauvin, M., Idrissi, N., Berdeaux, A. British journal of clinical pharmacology. (1977) [Pubmed]
  4. Usefulness of penbutolol for systemic hypertension. Penbutolol Research Group. Schoenberger, J.A. Am. J. Cardiol. (1989) [Pubmed]
  5. Absence of genotoxic activity of penbutolol in bacterial and mammalian cell screening systems. Müller, W., Cojocel, C., Kramer, W., Mayer, D. Mutat. Res. (1990) [Pubmed]
  6. The effect of single doses of penbutolol and propranolol L.A. on psychomotor performance. Broadhurst, A.D., Monaghan, A.T. British journal of clinical pharmacology. (1984) [Pubmed]
  7. Does a single priming injection of clenbuterol alter behavioral response to beta-adrenoceptor agonists and antagonists in mice through a time-dependent process? Martin, P., Soubrie, P., Simon, P. Eur. J. Pharmacol. (1985) [Pubmed]
  8. A comparative study of atenolol and penbutolol in hypertensive patients. Lameijer, L.D., Houtzagers, J.J., Voermans, L.A. Eur. Heart J. (1983) [Pubmed]
  9. Single and divided doses of penbutolol. Müller, F.O., Hundt, H.K., Bromley, P.A., Torres, J., Vanderbeke, O. Clin. Pharmacol. Ther. (1979) [Pubmed]
  10. Beta-2 adrenoceptor blocking activity of penbutolol and propranolol at very low doses. Kulkarni, R.D., DaSilva, L.M., Chabria, N.L., Chadha, D.R. Clin. Pharmacol. Ther. (1977) [Pubmed]
  11. Liquid-chromatographic determination of penbutolol and its principal metabolites in plasma and urine. Miner, D.J., Binkley, D.A., Bechtol, L.D. Clin. Chem. (1984) [Pubmed]
  12. A comparison of a combination of penbutolol and frusemide with the two compounds individually in the treatment of hypertension. Chadha, D.R., Houtzagers, J.J. British journal of clinical pharmacology. (1983) [Pubmed]
  13. Penbutolol and propranolol: a comparison of their effects on antipyrine clearance in man. Bax, N.D., Jones, R.W., Lennard, M.S., Tucker, G.T., Woods, H.F. British journal of clinical pharmacology. (1985) [Pubmed]
  14. Use of fixed doses of beta blocking drugs in the treatment of hypertension. Randomised study of atenolol and penbutolol. Lameijer, L.D., Voermans, L.A., Houtzagers, J.J., Chadha, D.R. Eur. J. Clin. Pharmacol. (1981) [Pubmed]
  15. Efficacy of penbutolol + piretanide combinations in the treatment of arterial hypertension. Verho, M., Rangoonwala, B., Pahnke, K., Freude, J., Häringer, E. Drugs under experimental and clinical research. (1985) [Pubmed]
  16. Long term treatment of moderate hypertension with penbutolol (Hoe 893d). II. Effect on the response of plasma catecholamines and plasma renin activity to insulin-induced hypoglycemia. Hansson, B.G., Hökfelt, n.u.l.l. Eur. J. Clin. Pharmacol. (1976) [Pubmed]
  17. The membrane stabilizing activity of beta-adrenoceptor ligands. Quantitative evaluation of the interaction of phenoxypropanolamines with the [3H]batrachotoxinin A 20-alpha-benzoate binding site on voltage-sensitive sodium channels in rat brain. Ijzerman, A.P., Nagesser, A., Garritsen, A. Biochem. Pharmacol. (1987) [Pubmed]
  18. Penbutolol in the treatment of mild to moderate essential hypertension in black South Africans. Venter, C.P., Joubert, P.H., Venter, H.L., Muntingh, G.L., du Plooy, W.J. Journal of clinical pharmacology. (1990) [Pubmed]
  19. Decrease in penbutolol protein binding as a consequence of treatment with some alkylating agents. Aguirre, C., Rodríguez-Sasiain, J.M., Calvo, R. Cancer Chemother. Pharmacol. (1994) [Pubmed]
  20. The uptake and overflow of radiolabelled beta-adrenoceptor blocking agents by the isolated vas deferens of the rat. Lewis, M.J. Br. J. Pharmacol. (1977) [Pubmed]
  21. DNA strand breaks and mutations caused by penbutolol, a beta blocker. Hussain, S.S., Al-Dakan, A.A., Aboul-Enein, H.Y., Hannan, M.A. Mutat. Res. (1988) [Pubmed]
  22. Penbutolol: beta-adrenoceptor interaction and the time course of plasma concentrations explain its prolonged duration of action in man. Wellstein, A., Palm, D. Eur. J. Clin. Pharmacol. (1985) [Pubmed]
  23. In vivo microdialysis evidence for central serotonin1A and serotonin1B autoreceptor blocking properties of the beta adrenoceptor antagonist (-)penbutolol. Hjorth, S., Sharp, T. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  24. Studies on the stereoisomers of beta-adrenoceptor antagonists in conscious A-V blocked dogs. Boucher, M., Duchêne-Marullaz, P., Moundanga, J.L. Br. J. Pharmacol. (1986) [Pubmed]
  25. Autoreceptor antagonists enhance the effect of the reuptake inhibitor citalopram on extracellular 5-HT: this effect persists after repeated citalopram treatment. Gundlah, C., Hjorth, S., Auerbach, S.B. Neuropharmacology (1997) [Pubmed]
  26. Plasma level studies of penbutolol after oral dose in man. Vallner, J.J., Jun, H.W., Needham, T.E., Stewart, J.T., Brown, W., Frazer, H., Honigberg, I.L. Journal of clinical pharmacology. (1977) [Pubmed]
  27. Prediction of metabolic drug interactions involving beta-adrenoceptor blocking drugs. Park, B.K. British journal of clinical pharmacology. (1984) [Pubmed]
  28. Increase in the isolation-induced social behavioural deficit by agonists at 5-HT1A receptors. Francès, H., Khidichian, F., Monier, C. Neuropharmacology (1990) [Pubmed]
  29. Penbutolol: a preliminary review of its pharmacological properties and therapeutic efficacy in hypertension and angina pectoris. Heel, R.C., Brogden, R.N., Speight, T.M., Avery, G.S. Drugs (1981) [Pubmed]
  30. Determination of penbutolol and its hydroxylated metabolite in biological fluids by reversed-phase high-performance liquid chromatography. Bernard, N., Cuisinaud, G., Sassard, J. J. Chromatogr. (1982) [Pubmed]
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