Skip to main content
PMC home page
British Journal of Clinical Pharmacology logoLink to British Journal of Clinical Pharmacology
. 1978 Jan;5(1):19–26. doi: 10.1111/j.1365-2125.1978.tb01593.x

Blockade of isoprenaline-induced changes in plasma free fatty acids, immunoreactive insulin levels and plasma renin activity in healthy human subjects, by propranolol, pindolol, practolol, atenolol, metoprolol and acebutolol

H H Harms, L Gooren, A J G Spoelstra, C Hesse, L Verschoor
PMCID: PMC1429223  PMID: 23133

Abstract

1 The effects of intravenously administered propranolol 0.01 and 0.03, pindolol 0.001 and 0.003, practolol 0.12 and 0.36, atenolol 0.03 and 0.09, metoprolol 0.045 and 0.135 and acebutolol 0.12 and 0.36 mg/kg, on isoprenaline-induced changes in heart rate, blood pressure, plasma free fatty acids, immunoreactive insulin plasma levels and plasma renin activity were determined in six healthy human subjects.

2 Propranolol, atenolol and metoprolol had a stronger effect on resting heart rate than practolol, acebutolol and pindolol, probably reflecting differences in intrinsic β-sympathomimetic activity. Antagonist potencies against isoprenaline-induced changes in heart rate and blood pressure suggested cardioselectivity for practolol, atenolol, metoprolol and the lower dose of acebutolol and non-cardioselectivity for propranolol, pindolol and the higher dose of acebutolol.

3 All six β-adrenoceptor blocking agents were able, to a varying extent, to antagonize the isoprenaline-induced increases in plasma free fatty acids and plasma immunoreactive insulin levels. In general, the cardioselective agents were relatively less effective antagonists than the non-cardioselective agents.

4 Resting plasma renin activity was reduced by all six β-adrenoceptor blocking agents, suggestive of the presence of β1-adrenoceptors mediating renin release, but the non-cardioselective agents propranolol and pindolol seemed relatively more effective in antagonizing isoprenaline-induced increases in plasma renin activity than the cardioselective agents, which indicates that β2-adrenoceptors might also be involved.

5 The results are compatible with the hypothesis that both β1- and β2-adrenoceptors are involved in the regulation of lipolysis, insulin release and renin release.

Full text

PDF
19

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Ablad B., Borg K. O., Carlsson E., EK L., Johnson G., Malmfors T., Regårdh C. G. A survey of the pharmacological properties of metoprolol in animals and man. Acta Pharmacol Toxicol (Copenh) 1975;36(Suppl 5):7–23. doi: 10.1111/j.1600-0773.1975.tb03318.x. [DOI] [PubMed] [Google Scholar]
  2. Aström H., Vallin H. Effect of a new beta-adrenergic blocking agent, ICI 66o82, on exercise haemodynamics and airway resistance in angina pectoris. Br Heart J. 1974 Dec;36(12):1194–1200. doi: 10.1136/hrt.36.12.1194. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Basil B., Jordan R., Loveless A. H., Maxwell D. R. Beta-adrenoceptor blocking properties and cardioselectivity of M & B 17,803A. Br J Pharmacol. 1973 Jun;48(2):198–211. doi: 10.1111/j.1476-5381.1973.tb06906.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Bühler F. R., Burkart F., Lütold B. E., Küng M., Marbet G., Pfisterer M. Antihypertensive beta blocking action as related to renin and age: a pharmacologic tool to identify pathogenetic mechanisms in essential hypertension. Am J Cardiol. 1975 Oct 31;36(5):653–669. doi: 10.1016/0002-9149(75)90168-x. [DOI] [PubMed] [Google Scholar]
  5. De Plaen J. F., Amery A., Reybrouck T. Comparative potency of atenolol and propranolol as beta-adrenergic blocking agents in man. Eur J Clin Pharmacol. 1976 Sep 30;10(5):297–303. doi: 10.1007/BF00565617. [DOI] [PubMed] [Google Scholar]
  6. Gibbons D. O., Lant A. F., Ashford A., Collins R. F., Pinder S. Comparative effects of acebutolol and practolol on the lipolytic response to isoprenaline. Br J Clin Pharmacol. 1976 Feb;3(1):177–184. doi: 10.1111/j.1365-2125.1976.tb00586.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  7. Goldberg R., van As M., Joffe B. I., Krut L., Bersohn I., Seftel H. C. Metabolic responses to selective beta-adrenergic stimulation in man. Postgrad Med J. 1975 Feb;51(592):53–58. doi: 10.1136/pgmj.51.592.53. [DOI] [PMC free article] [PubMed] [Google Scholar]
  8. Harms H. H. Isoproterenol antagonism of cardioselective beta adrenergic receptor blocking agents: a comparative study of human and guinea-pig cardiac and bronchial beta adrenergic receptors. J Pharmacol Exp Ther. 1976 Nov;199(2):329–335. [PubMed] [Google Scholar]
  9. Harms H. H. Stereochemical aspects of beta-adrenoceptor antagonist-receptor interaction in adipocytes. Differentiation of beta-adrenoceptors in human and rat adipocytes. Life Sci. 1976 Nov 1;19(9):1447–1452. doi: 10.1016/0024-3205(76)90447-1. [DOI] [PubMed] [Google Scholar]
  10. Harms H. H., Van der Meer J. Isoprenaline antagonism of cardioselective beta-adrenergic receptor blocking agents on human and rat adipocytes. Br J Clin Pharmacol. 1975 Aug;2(4):311–315. doi: 10.1111/j.1365-2125.1975.tb02776.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Harms H. H., Zaagsma J., Van der Wal B. Beta-adrenoceptor studies. III. On the beta-adrenoceptors in rat adipose tissue. Eur J Pharmacol. 1974 Jan;25(1):87–91. doi: 10.1016/0014-2999(74)90098-3. [DOI] [PubMed] [Google Scholar]
  12. Imura H., Kato Y., Ikeda M., Morimoto M., Yawata M. Effect of adrenergic-blocking or -stimulating agents on plasma growth hormone, immunoreactive insulin, and blood free fatty acid levels in man. J Clin Invest. 1971 May;50(5):1069–1079. doi: 10.1172/JCI106578. [DOI] [PMC free article] [PubMed] [Google Scholar]
  13. Johnsson G., Nyberg G., Sölvell L. Influence of metoprolol and propranolol on hemodynamic effects induced by physical work and isoprenaline. Acta Pharmacol Toxicol (Copenh) 1975;36(Suppl 5):69–75. doi: 10.1111/j.1600-0773.1975.tb03323.x. [DOI] [PubMed] [Google Scholar]
  14. Ko H., Royer M. E. A submicromolar assay for nonpolar acids in plasma and depot fat. Anal Biochem. 1967 Aug;20(2):205–214. doi: 10.1016/0003-2697(67)90026-7. [DOI] [PubMed] [Google Scholar]
  15. Lands A. M., Arnold A., McAuliff J. P., Luduena F. P., Brown T. G., Jr Differentiation of receptor systems activated by sympathomimetic amines. Nature. 1967 May 6;214(5088):597–598. doi: 10.1038/214597a0. [DOI] [PubMed] [Google Scholar]
  16. Lehfeldt D. C., Hutchens T. T. A kinetic method for determination of plasma renin activity using radioassay of Angiotensin I. Am J Clin Pathol. 1971 May;55(5):513–522. doi: 10.1093/ajcp/55.5.513. [DOI] [PubMed] [Google Scholar]
  17. Loubatières A., Mariani M. M., Sorel G., Savi L. The action of beta-adrenergic blocking and stimulating agents on insulin secretion. Characterization of the type of beta receptor. Diabetologia. 1971 Jun;7(3):127–132. doi: 10.1007/BF01212541. [DOI] [PubMed] [Google Scholar]
  18. Rowe M. J., Neilson J. M., Oliver M. F. Control of ventricular arrhythmias during myocardial infarction by antilipolytic treatment using a nicotinic-acid analogue. Lancet. 1975 Feb 8;1(7902):295–300. doi: 10.1016/s0140-6736(75)91206-4. [DOI] [PubMed] [Google Scholar]
  19. Wilson A. G., Brooke O. G., Lloyd H. J., Robinson B. F. Mechanism of action of beta-adrenergic receptor blocking agents in angina pectoris: comparison of action of propranolol with dexpropranolol and practolol. Br Med J. 1969 Nov 15;4(5680):399–401. doi: 10.1136/bmj.4.5680.399. [DOI] [PMC free article] [PubMed] [Google Scholar]
  20. YALOW R. S., BERSON S. A. Immunoassay of endogenous plasma insulin in man. J Clin Invest. 1960 Jul;39:1157–1175. doi: 10.1172/JCI104130. [DOI] [PMC free article] [PubMed] [Google Scholar]

Articles from British Journal of Clinical Pharmacology are provided here courtesy of British Pharmacological Society

RESOURCES