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
Molecular Pharmacology
  • 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
Molecular Pharmacology

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 molpharm on Facebook
  • Follow molpharm on Twitter
  • Follow molpharm on LinkedIn
Research ArticleArticle

Mathematical Analysis of the Kinetics of Competitive Inhibition in Neurotransmitter Receptor Binding Assays

FREDERICK J. EHLERT, WILLIAM R. ROESKE and HENRY I. YAMAMURA
Molecular Pharmacology May 1981, 19 (3) 367-371;
FREDERICK J. EHLERT
Departments of Pharmacology, Psychiatry, and Internal Medicine, University of Arizona Health Sciences Center, Tucson, Arizona 85724
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
WILLIAM R. ROESKE
Departments of Pharmacology, Psychiatry, and Internal Medicine, University of Arizona Health Sciences Center, Tucson, Arizona 85724
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
HENRY I. YAMAMURA
Departments of Pharmacology, Psychiatry, and Internal Medicine, University of Arizona Health Sciences Center, Tucson, Arizona 85724
  • 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

The kinetics of competitive inhibition was described by first-order differential equations, and the solution to these equations was derived numerically. The results of this analysis showed that the IC50 of a competitive inhibition curve decreases as equilibrium is approached if the dissociation rate constant of the nonlabeled ligand is equal to or less than that of the labeled ligand. The converse was true for competitive inhibition curves of a nonlabeled inhibitor with a dissociation rate constant greater than that of the labeled ligand. Nonequilibrium competitive inhibition experiments were performed using the muscarinic antagonist and agonist ligands, [3H]quinuclidinyl benzilate and [3H]cis-methyldioxolane, and results consistent with the theoretical predictions were observed.

ACKNOWLEDGMENTS The authors wish to thank Susan Yamamura for her expert appraisal of the manuscript. We also acknowledge the expert technical assistance of David Chapman and the excellent secretarial assistance of Cathleen Thomas and Isabelle Preiss.

  • Copyright © 1981 by The American Society for Pharmacology and Experimental Therapeutics

MolPharm 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

Molecular Pharmacology
Vol. 19, Issue 3
1 May 1981
  • 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 Molecular Pharmacology 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.
Mathematical Analysis of the Kinetics of Competitive Inhibition in Neurotransmitter Receptor Binding Assays
(Your Name) has forwarded a page to you from Molecular Pharmacology
(Your Name) thought you would be interested in this article in Molecular Pharmacology.
CAPTCHA
This question is for testing whether or not you are a human visitor and to prevent automated spam submissions.
Citation Tools
Research ArticleArticle

Mathematical Analysis of the Kinetics of Competitive Inhibition in Neurotransmitter Receptor Binding Assays

FREDERICK J. EHLERT, WILLIAM R. ROESKE and HENRY I. YAMAMURA
Molecular Pharmacology May 1, 1981, 19 (3) 367-371;

Citation Manager Formats

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

Share
Research ArticleArticle

Mathematical Analysis of the Kinetics of Competitive Inhibition in Neurotransmitter Receptor Binding Assays

FREDERICK J. EHLERT, WILLIAM R. ROESKE and HENRY I. YAMAMURA
Molecular Pharmacology May 1, 1981, 19 (3) 367-371;
del.icio.us logo Digg logo Reddit logo Twitter logo Facebook logo Google logo Mendeley logo
  • Tweet Widget
  • Facebook Like
  • Google Plus One

Jump to section

  • Article
  • Info & Metrics
  • eLetters
  • PDF

Related Articles

Cited By...

More in this TOC Section

  • The binding site for KCI807 in the androgen receptor
  • Fatty acid amide hydrolase in cisplatin nephrotoxicity
  • eCB Signaling System in hiPSC-Derived Neuronal Cultures
Show more Article

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 Molecular Pharmacology
  • 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
  • Journal of Pharmacology and Experimental Therapeutics
  • Pharmacological Reviews
  • Pharmacology Research & Perspectives
ISSN 1521-0111 (Online)

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