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

Inhibition of amino acid transport by nonsteroidal anti-inflammatory drugs: a model for predicting relative therapeutic potency.

G F Seng and B M Bayer
Journal of Pharmacology and Experimental Therapeutics May 1986, 237 (2) 496-503;
G F Seng
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
B M Bayer
  • 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

Indomethacin has been shown to inhibit selectively the rate of alpha-(methylamino)-isobutyric acid (MeAIB) uptake by the "A" transport system in several cell types. This study was undertaken to determine if this activity was shared by other nonsteroidal anti-inflammatory drugs (NSAID), if the inhibition of MeAIB transport was unique to drugs with anti-inflammatory activity and finally if it could be correlated with their in vivo potency in humans and in animal test systems. Utilizing BRLT rat hepatocyte cultures (hepatocytes cloned from Buffalo rats); it was found that all of the acidic NSAID tested inhibited MeAIB uptake in a dose-dependent manner with IC50 values in the low to midmicromolar range. The amount of inhibition was dependent on cell density, time of incubation with drug, the media pH and its concentration of protein and amino acids. The order of potency of the acidic NSAID in inhibiting MeAIB uptake was found to be correlated closely with their potency in the inhibition of prostaglandin synthesis in vitro, the suppression of induced inflammatory reactions in rats and the maximum recommended daily doses in humans. Pharmacologically inactive metabolites of several NSAID had little or no effect on MeAIB transport at concentrations up to 10 times greater than active parent compounds. Other compounds tested, including glucocorticoids, were found to have little effect on the rate of MeAIB uptake. These studies indicate that the inhibition of MeAIB uptake in BRLT cells may represent a reliable and rapid screen for predicting the therapeutic potency of newly developed NSAID.

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. 237, Issue 2
1 May 1986
  • 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.
Inhibition of amino acid transport by nonsteroidal anti-inflammatory drugs: a model for predicting relative therapeutic potency.
(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

Inhibition of amino acid transport by nonsteroidal anti-inflammatory drugs: a model for predicting relative therapeutic potency.

G F Seng and B M Bayer
Journal of Pharmacology and Experimental Therapeutics May 1, 1986, 237 (2) 496-503;

Citation Manager Formats

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

Share
Abstract

Inhibition of amino acid transport by nonsteroidal anti-inflammatory drugs: a model for predicting relative therapeutic potency.

G F Seng and B M Bayer
Journal of Pharmacology and Experimental Therapeutics May 1, 1986, 237 (2) 496-503;
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