Skip to main content
British Journal of Clinical Pharmacology logoLink to British Journal of Clinical Pharmacology
. 1987 Sep;24(3):397–399. doi: 10.1111/j.1365-2125.1987.tb03188.x

A method for estimating the potency of angiotensin-converting enzyme inhibitors in man.

A Wellstein 1, J Essig 1, G G Belz 1
PMCID: PMC1386265  PMID: 2959304

Abstract

Dose-response curves of the effect of angiotensin I (A-I) infusion on diastolic blood pressure were constructed before and 3 h following single oral doses of the angiotensin-converting enzyme (ACE) inhibitor cilazapril (1.25 to 30 mg) in six normal male subjects. Cilazapril shifted the A-I dose-response curves dose dependently rightward; Schild-plot analysis indicated a competitive antagonism by cilazapril with an apparent Ki-dose of about 0.6 mg.

Full text

PDF
397

Selected References

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

  1. ARUNLAKSHANA O., SCHILD H. O. Some quantitative uses of drug antagonists. Br J Pharmacol Chemother. 1959 Mar;14(1):48–58. doi: 10.1111/j.1476-5381.1959.tb00928.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Belz G. G., Essig J., Wellstein A. Hemodynamic responses to angiotensin I in normal volunteers and the antagonism by the angiotensin-converting enzyme inhibitor cilazapril. J Cardiovasc Pharmacol. 1987 Feb;9(2):219–224. doi: 10.1097/00005344-198702000-00015. [DOI] [PubMed] [Google Scholar]
  3. Belz G. G., Lange H., Tschollar W., Neis W. Cilazapril bei essentieller Hypertonie. Eine placebokontrollierte Doppelblindstudie zur Dosisfindung. Med Klin (Munich) 1986 Jul 18;81(15-16):524–529. [PubMed] [Google Scholar]
  4. GADDUM J. H. Theories of drug antagonism. Pharmacol Rev. 1957 Jun;9(2):211–218. [PubMed] [Google Scholar]
  5. Hassall C. H., Kröhn A., Moody C. J., Thomas W. A. The design of a new group of angiotensin-converting enzyme inhibitors. FEBS Lett. 1982 Oct 18;147(2):175–179. doi: 10.1016/0014-5793(82)81036-3. [DOI] [PubMed] [Google Scholar]
  6. Natoff I. L., Nixon J. S., Francis R. J., Klevans L. R., Brewster M., Budd J., Patel A. T., Wenger J., Worth E. Biological properties of the angiotensin-converting enzyme inhibitor cilazapril. J Cardiovasc Pharmacol. 1985 May-Jun;7(3):569–580. doi: 10.1097/00005344-198505000-00025. [DOI] [PubMed] [Google Scholar]
  7. Ondetti M. A., Cushman D. W. Enzymes of the renin-angiotensin system and their inhibitors. Annu Rev Biochem. 1982;51:283–308. doi: 10.1146/annurev.bi.51.070182.001435. [DOI] [PubMed] [Google Scholar]
  8. STEPHENSON R. P. A modification of receptor theory. Br J Pharmacol Chemother. 1956 Dec;11(4):379–393. doi: 10.1111/j.1476-5381.1956.tb00006.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Strittmatter S. M., Snyder S. H. Characterization of angiotensin converting enzyme by [3H]captopril binding. Mol Pharmacol. 1986 Feb;29(2):142–148. [PubMed] [Google Scholar]
  10. Wellstein A., Palm D., Pitschner H. F., Belz G. G. Receptor binding of propranolol is the missing link between plasma concentration kinetics and the effect-time course in man. Eur J Clin Pharmacol. 1985;29(2):131–147. doi: 10.1007/BF00547412. [DOI] [PubMed] [Google Scholar]

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

RESOURCES