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

AN INVESTIGATION OF THE MOLECULAR CONFIGURATIONS FAVORABLE FOR STIMULATION OR BLOCKADE OF THE ACETYLCHOLINE-SENSITIVE RECEPTORS OF VISCERAL ORGANS

A. M. Lands
Journal of Pharmacology and Experimental Therapeutics August 1951, 102 (4) 219-236;
A. M. Lands
  • 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. A large variety of structurally diverse molecules are capable of reacting with the acetylcholine sensitive receptor of the heart and intestine and thereby inducing stimulation (cholinemimetic action). The most effective compounds have at least one methyl group in the cationic head and a terminal methyl group at a distance of about 7 Å. No structural elements other than C, H and N are required for this action.

2. The acetate esters of 1-methyl-3-piperidylmethanol are weak cholinemimetic agents.

3. Substitution of the terminal methane by aromatic, heterocyclic, cycloalkyl and/or an hydroxyl abolishes cholinemimetic action and the resultant molecule is an active cholinolytic agent. Evidence is presented suggesting that blockade results from the saturation of the receptor surface with inactive molecules.

4. The distance between the N and the substituted terminal methane does not appear to be critical but this distance is 4-8 Å for the most active cholinolytic agents.

5. Various derivatives of 1-methylpiperidine have cholinolytic activities of the same order of magnitude as that of atropine. It is suggested that the methylpiperidine ring is the essential part of tropine.

Footnotes

    • Received April 27, 1951.

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. 102, Issue 4
1 Aug 1951
  • Table of Contents
  • Table of Contents (PDF)
  • Index by author
  • Back Matter (PDF)
  • 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.
AN INVESTIGATION OF THE MOLECULAR CONFIGURATIONS FAVORABLE FOR STIMULATION OR BLOCKADE OF THE ACETYLCHOLINE-SENSITIVE RECEPTORS OF VISCERAL ORGANS
(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

AN INVESTIGATION OF THE MOLECULAR CONFIGURATIONS FAVORABLE FOR STIMULATION OR BLOCKADE OF THE ACETYLCHOLINE-SENSITIVE RECEPTORS OF VISCERAL ORGANS

A. M. Lands
Journal of Pharmacology and Experimental Therapeutics August 1, 1951, 102 (4) 219-236;

Citation Manager Formats

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

Share
Research ArticleArticle

AN INVESTIGATION OF THE MOLECULAR CONFIGURATIONS FAVORABLE FOR STIMULATION OR BLOCKADE OF THE ACETYLCHOLINE-SENSITIVE RECEPTORS OF VISCERAL ORGANS

A. M. Lands
Journal of Pharmacology and Experimental Therapeutics August 1, 1951, 102 (4) 219-236;
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

  • PST3093 Stimulates SERCA2a and Improves Cardiac Function
  • CRV431 Decreases Liver Fibrosis and Tumor Development
  • Pharmacological Characterization of Nicotine-Induced Seizures in Mice
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 © 2023 by the American Society for Pharmacology and Experimental Therapeutics