Skip to main content
Advertisement

Main menu

  • Home
  • Articles
    • Current Issue
    • Fast Forward
    • Latest Articles
    • Special Sections
    • Archive
  • Information
    • Instructions to Authors
    • Submit a Manuscript
    • FAQs
    • For Subscribers
    • Terms & Conditions of Use
    • Permissions
  • Editorial Board
  • Alerts
    • Alerts
    • RSS Feeds
  • Virtual Issues
  • Feedback
  • Submit
  • Other Publications
    • Drug Metabolism and Disposition
    • Journal of Pharmacology and Experimental Therapeutics
    • Molecular Pharmacology
    • Pharmacological Reviews
    • Pharmacology Research & Perspectives
    • ASPET

User menu

  • My alerts
  • Log in
  • My Cart

Search

  • Advanced search
Journal of Pharmacology and Experimental Therapeutics
  • Other Publications
    • Drug Metabolism and Disposition
    • Journal of Pharmacology and Experimental Therapeutics
    • Molecular Pharmacology
    • Pharmacological Reviews
    • Pharmacology Research & Perspectives
    • ASPET
  • My alerts
  • Log in
  • My Cart
Journal of Pharmacology and Experimental Therapeutics

Advanced Search

  • Home
  • Articles
    • Current Issue
    • Fast Forward
    • Latest Articles
    • Special Sections
    • Archive
  • Information
    • Instructions to Authors
    • Submit a Manuscript
    • FAQs
    • For Subscribers
    • Terms & Conditions of Use
    • Permissions
  • Editorial Board
  • Alerts
    • Alerts
    • RSS Feeds
  • Virtual Issues
  • Feedback
  • Submit
  • Visit jpet on Facebook
  • Follow jpet on Twitter
  • Follow jpet on LinkedIn
Abstract

Oxidation of (R)- and (S)-propranolol in human and dog liver microsomes. Species differences in stereoselectivity.

C von Bahr, J Hermansson and M Lind
Journal of Pharmacology and Experimental Therapeutics August 1982, 222 (2) 458-462;
C von Bahr
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
J Hermansson
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
M Lind
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
  • Article
  • Info & Metrics
  • eLetters
  • PDF
Loading

Abstract

Propranolol is an adrenergic beta receptor antagonist whose kinetics is complicated by dose-dependency, formation of active metabolites and stereoselective availability. To get some insight of the possible metabolic factors behind this, we have incubated the two optical isomers (R)- and (S)-propranolol with human and dog liver microsomes. Propranolol and its oxidized metabolites 4-hydroxypropranolol (4-OH-P) and N-desisopropylpropranolol (nor-P) were analyzed using high-performance liquid chromatography and fluorometric detection. The oxidation rates varied markedly between human livers. Most of metabolized propranolol was recovered as 4-OH-P and nor-P and more propranolol was oxidized than glucuronidated. Formation rates of 4-OH-P and nor-P were approximately half-maximal at propranolol concentrations than can occur in the liver in vivo. The ratio between formation of these metabolites varied markedly between livers. Human livers formed 4-OH-P and nor-P most rapidly from (R)-propranolol, whereas dog livers formed 4-OH-P most rapidly from (S)-propranolol. We suggest that the interindividual differences in the capacity of the livers to metabolize propranolol largely should contribute to the kinetic variations observed between patients in vivo and the gradual saturation of 4-hydroxylation and N-desisopropylation of propranolol are likely to contribute to the dose-dependent kinetics.

JPET articles become freely available 12 months after publication, and remain freely available for 5 years. 

Non-open access articles that fall outside this five year window are available only to institutional subscribers and current ASPET members, or through the article purchase feature at the bottom of the page. 

 

  • Click here for information on institutional subscriptions.
  • Click here for information on individual ASPET membership.

 

Log in using your username and password

Forgot your user name or password?

Purchase access

You may purchase access to this article. This will require you to create an account if you don't already have one.
PreviousNext
Back to top

In this issue

Journal of Pharmacology and Experimental Therapeutics
Vol. 222, Issue 2
1 Aug 1982
  • Table of Contents
  • Table of Contents (PDF)
  • Index by author
  • Back Matter (PDF)
  • Editorial Board (PDF)
  • Front Matter (PDF)
Download PDF
Article Alerts
Sign In to Email Alerts with your Email Address
Email Article

Thank you for sharing this Journal of Pharmacology and Experimental Therapeutics article.

NOTE: We request your email address only to inform the recipient that it was you who recommended this article, and that it is not junk mail. We do not retain these email addresses.

Enter multiple addresses on separate lines or separate them with commas.
Oxidation of (R)- and (S)-propranolol in human and dog liver microsomes. Species differences in stereoselectivity.
(Your Name) has forwarded a page to you from Journal of Pharmacology and Experimental Therapeutics
(Your Name) thought you would be interested in this article in Journal of Pharmacology and Experimental Therapeutics.
CAPTCHA
This question is for testing whether or not you are a human visitor and to prevent automated spam submissions.
Citation Tools
Abstract

Oxidation of (R)- and (S)-propranolol in human and dog liver microsomes. Species differences in stereoselectivity.

C von Bahr, J Hermansson and M Lind
Journal of Pharmacology and Experimental Therapeutics August 1, 1982, 222 (2) 458-462;

Citation Manager Formats

  • BibTeX
  • Bookends
  • EasyBib
  • EndNote (tagged)
  • EndNote 8 (xml)
  • Medlars
  • Mendeley
  • Papers
  • RefWorks Tagged
  • Ref Manager
  • RIS
  • Zotero

Share
Abstract

Oxidation of (R)- and (S)-propranolol in human and dog liver microsomes. Species differences in stereoselectivity.

C von Bahr, J Hermansson and M Lind
Journal of Pharmacology and Experimental Therapeutics August 1, 1982, 222 (2) 458-462;
Reddit logo Twitter logo Facebook logo Mendeley logo
  • Tweet Widget
  • Facebook Like
  • Google Plus One

Jump to section

  • Article
  • Info & Metrics
  • eLetters
  • PDF

Related Articles

Cited By...

Similar Articles

Advertisement
  • Home
  • Alerts
Facebook   Twitter   LinkedIn   RSS

Navigate

  • Current Issue
  • Fast Forward by date
  • Fast Forward by section
  • Latest Articles
  • Archive
  • Search for Articles
  • Feedback
  • ASPET

More Information

  • About JPET
  • Editorial Board
  • Instructions to Authors
  • Submit a Manuscript
  • Customized Alerts
  • RSS Feeds
  • Subscriptions
  • Permissions
  • Terms & Conditions of Use

ASPET's Other Journals

  • Drug Metabolism and Disposition
  • Molecular Pharmacology
  • Pharmacological Reviews
  • Pharmacology Research & Perspectives
ISSN 1521-0103 (Online)

Copyright © 2023 by the American Society for Pharmacology and Experimental Therapeutics