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

Studies on Histamine H2 Receptors Coupled to Cardiac Adenylate Cyclase

Blockade by H2 and H1 Receptor Antagonists

CARL L. JOHNSON, HAREL WEINSTEIN and JACK PETER GREEN
Molecular Pharmacology September 1979, 16 (2) 417-428;
CARL L. JOHNSON
Department of Pharmacology and Cell Biophysics, University of Cincinnati College of Medicine, 231 Bethesda Avenue, Cincinnati, Ohio 45267
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
HAREL WEINSTEIN
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
JACK PETER GREEN
  • 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

In particulate preparations from guinea pig ventricle, histamine caused a three to five-fold stimulation of basal adenylate cyclase activity. The H2 antagonist, cimetidine, displaced the dose-response curve of histamine to the right in a parallel fashion suggesting competitive antagonism. Schild plots were linear with slopes near one, consistent with a competitive inhibition mechanism. The affinity of cimetidine was independent of whether histamine or the pure H2 agonist dimaprit was used to activate the enzyme. A series of ten H2 antagonists related to cimetidine were examined for inhibition of histamine-stimulated cyclase activity. An excellent correlation was found between the affinities of these compounds for the H2 linked cyclase system and for physiological H2 receptors. Although several H1 antagonists also appeared to be competitive inhibitors of the histamine-activated cyclase, their affinities did not correlate with data for H1 receptors in the guinea pig ileum. The affinities of the antagonists, both H2 and H1, on the cardiac adenylate cyclase were virtually identical to their affinities for a histamine-stimulated cyclase from brain. The results suggest that the histamine-sensitive adenylate cyclase in ventricular muscle quantitatively retains the properties of an H2 receptor system as defined physiologically and that the histamine receptors in ventricle and brain are not distinguishable. This study provides further strong evidence that histamine's inotropic and chronotropic effects on the intact heart are mediated by cAMP through H2 receptor activation.

ACKNOWLEDGMENT The authors extend their sincere appreciation to Dr. C. R. Ganellin (Smith Kline and French Laboratories, England) for his generous gift of the H2 antagonists used in this study and to Drs. Kanof and Greengard for sending us their manuscripts prior to publication.

  • Copyright © 1979 by Academic Press, Inc.

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. 16, Issue 2
1 Sep 1979
  • Table of Contents
  • Table of Contents (PDF)
  • Index by author
  • Editorial Board (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.
Studies on Histamine H2 Receptors Coupled to Cardiac Adenylate Cyclase
(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

Studies on Histamine H2 Receptors Coupled to Cardiac Adenylate Cyclase

CARL L. JOHNSON, HAREL WEINSTEIN and JACK PETER GREEN
Molecular Pharmacology September 1, 1979, 16 (2) 417-428;

Citation Manager Formats

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

Share
Research ArticleArticle

Studies on Histamine H2 Receptors Coupled to Cardiac Adenylate Cyclase

CARL L. JOHNSON, HAREL WEINSTEIN and JACK PETER GREEN
Molecular Pharmacology September 1, 1979, 16 (2) 417-428;
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...

More in this TOC Section

  • Fatty Acid Amide Hydrolase in Cisplatin Nephrotoxicity
  • Use-Dependent Relief of A-887826 Inhibition
  • Benzbromarone Relaxes Airway Smooth Muscle via BK Activation
Show more Articles

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