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
Research ArticleArticle

ANTISPASMODIC ACTIVITY OF BASIC ESTERS AND QUATERNARY DERIVATIVES OF β-HYDROXY ACIDS

Melvin H. Ehrenberg, J. A. Ramp, E. W. Blanchard and G. R. Treves
Journal of Pharmacology and Experimental Therapeutics October 1952, 106 (2) 141-156;
Melvin H. Ehrenberg
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
J. A. Ramp
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
E. W. Blanchard
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
G. R. Treves
  • 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

1. Thirty-eight synthetic compounds, all of them esters of disubstituted acetic acids, have been tested for anticholinergic activity against acetylcholine-stimulated ileal strips. One of them (158) proved superior to, and two of them (154, 96) proved equal to atropine in activity. The quaternary alkamines were generally more potent than their corresponding tertiary alkamines. Two compounds (79, 95) also exhibited significant antispasmodic action against barium chloride induced contractures in vitro.

2. Five of the more active compounds were tested in the cat for atropine-like action on the intact intestines, and on salivary flow in the rabbit. One compound (158), whose spasmolytic effects were superior to atropine both in vitro and in vivo, exhibited ¾ of the inhibitory effect of atropine on salivary secretion.

3. Eight compounds were tested for anticholinergic activity on blood pressure.

4. The paralellism between the antagonism of drugs to nicotine-induced tremors and the satisfactory clinical use of these drugs in the alleviation of Parkinson's symptomatology has been discussed. Compound 93 afforded complete protection against nicotine-induced tremors on intravenous administration, and partial protection by oral administration.

5. The toxicity of the compounds was presented in comparison with presently used antispasmodic agents. In general, the quaternary methosalts were approximately four times as toxic as the tertiary amines. Chronic toxicity studies gave no indication of any pathological changes in essential organs.

6. Mydriatic activity was tested in rabbits. The quaternary methohalides caused incomplete mydriasis in all cases tried. The tertiary compounds proved to be satisfactory mydriatics, in the laboratory, and are now undergoing clinical trial.

7. The relationship between chemical structure and pharmacological activity has been discussed.

Footnotes

    • Received May 26, 1952.

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. 106, Issue 2
1 Oct 1952
  • 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 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.
ANTISPASMODIC ACTIVITY OF BASIC ESTERS AND QUATERNARY DERIVATIVES OF β-HYDROXY ACIDS
(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
Research ArticleArticle

ANTISPASMODIC ACTIVITY OF BASIC ESTERS AND QUATERNARY DERIVATIVES OF β-HYDROXY ACIDS

Melvin H. Ehrenberg, J. A. Ramp, E. W. Blanchard and G. R. Treves
Journal of Pharmacology and Experimental Therapeutics October 1, 1952, 106 (2) 141-156;

Citation Manager Formats

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

Share
Research ArticleArticle

ANTISPASMODIC ACTIVITY OF BASIC ESTERS AND QUATERNARY DERIVATIVES OF β-HYDROXY ACIDS

Melvin H. Ehrenberg, J. A. Ramp, E. W. Blanchard and G. R. Treves
Journal of Pharmacology and Experimental Therapeutics October 1, 1952, 106 (2) 141-156;
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

  • CRV431 Decreases Liver Fibrosis and Tumor Development
  • Allosteric Modulation and Accelerated Resensitization of Human P2X3 Receptors by Cibacron Blue
  • Meeting Report for the ASPET–Ray Fuller Symposium: Cellular Mechanisms and Novel Strategies for Pain Control
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 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 © 2022 by the American Society for Pharmacology and Experimental Therapeutics