Skip to main content
Advertisement

Main menu

  • Home
  • Articles
    • Current Issue
    • Fast Forward
    • Latest Articles
    • 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
  • 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
    • 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
  • Visit molpharm on Facebook
  • Follow molpharm on Twitter
  • Follow molpharm on LinkedIn
Research ArticleArticle

4-(3-Cyclopentyloxy-4-methoxyphenyl)-2-pyrrolidone (ZK 62711): a Potent Inhibitor of Adenosine Cyclic 3',5'-Monophosphate Phosphodiesterases in Homogenates and Tissue Slices from Rat Brain

U. SCHWABE, M. MIYAKE, Y. OHGA and J. W. DALY
Molecular Pharmacology November 1976, 12 (6) 900-910;
U. SCHWABE
Laboratory of Chemistry, National Instiute of Arthritis, Metabolism, and Digestive Diseases, National Institutes of Health, Bethesda, Maryland 20014
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
M. MIYAKE
Laboratory of Chemistry, National Instiute of Arthritis, Metabolism, and Digestive Diseases, National Institutes of Health, Bethesda, Maryland 20014
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Y. OHGA
Laboratory of Chemistry, National Instiute of Arthritis, Metabolism, and Digestive Diseases, National Institutes of Health, Bethesda, Maryland 20014
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
J. W. DALY
Laboratory of Chemistry, National Instiute of Arthritis, Metabolism, and Digestive Diseases, National Institutes of Health, Bethesda, Maryland 20014
  • 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

A new class of inhibitor of phosphodiesterases is represented by 4-(3-cyclopentyloxy-4-methoxyphenyl)-2-pyrrolidone (ZK 62711). This compound enhances the magnitude of accumulations of cyclic 3',5'-AMP elicited by norepinephrine, isoproterenol, histamine, and adenosine in rat cerebral cortical slices and by veratridine in rat cerebellar slices and, in addition, increases basal levels of cyclic AMP in both cortical and cerebellar slices. Increases in intracellular levels of cyclic AMP in brain slices elicited by ZK 62711 do not appear to involve enhanced "release" of adenosine, since both basal and norepinephrine-elicited accumulations of cyclic AMP are increased by ZK 62711 in the presence of exogenous adenosine deaminase. ZK 62711 has little effect on levels of cyclic GMP in cortical or cerebellar slices. In rat cerebral homogenates ZK 62711 inhibits soluble and particulate cyclic AMP phosphodiesterases but is less potent with respect to cyclic GMP phosphodiesterases. At low concentrations it is 100 times more potent than a structurally related phosphodiesterase inhibitor, Ro 20-1724, with respect to the calcium-dependent cyclic AMP phosphodiesterase, and in brain slices it is similarly 100 times more potent in enhancing accumulations of cyclic AMP elicited by norepinephrine.

  • Copyright © 1976 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. 12, Issue 6
1 Nov 1976
  • 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 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.
4-(3-Cyclopentyloxy-4-methoxyphenyl)-2-pyrrolidone (ZK 62711): a Potent Inhibitor of Adenosine Cyclic 3',5'-Monophosphate Phosphodiesterases in Homogenates and Tissue Slices from Rat Brain
(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

4-(3-Cyclopentyloxy-4-methoxyphenyl)-2-pyrrolidone (ZK 62711): a Potent Inhibitor of Adenosine Cyclic 3',5'-Monophosphate Phosphodiesterases in Homogenates and Tissue Slices from Rat Brain

U. SCHWABE, M. MIYAKE, Y. OHGA and J. W. DALY
Molecular Pharmacology November 1, 1976, 12 (6) 900-910;

Citation Manager Formats

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

4-(3-Cyclopentyloxy-4-methoxyphenyl)-2-pyrrolidone (ZK 62711): a Potent Inhibitor of Adenosine Cyclic 3',5'-Monophosphate Phosphodiesterases in Homogenates and Tissue Slices from Rat Brain

U. SCHWABE, M. MIYAKE, Y. OHGA and J. W. DALY
Molecular Pharmacology November 1, 1976, 12 (6) 900-910;
del.icio.us logo Digg logo Reddit logo Twitter logo CiteULike 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

  • CTS bias
  • Nelfinavir and PXR
  • P2X7 Positive Modulator Structure-Activity Relationship
Show more Article

Similar Articles

  • 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 © 2021 by the American Society for Pharmacology and Experimental Therapeutics