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 ArticleGASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL

Inhibition of Human and Pig Ureter Motility in Vitro and in Vivo by the K+ Channel Openers PKF 217-744b and Nicorandil

Ruth Weiss, Meike Mevissen, Daniela S. Hauser, Günter Scholtysik, Christopher J. Portier, Bernhard Walter, Urs E. Studer and Hansjörg Danuser
Journal of Pharmacology and Experimental Therapeutics August 2002, 302 (2) 651-658; DOI: https://doi.org/10.1124/jpet.302.2.651
Ruth Weiss
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Meike Mevissen
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Daniela S. Hauser
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Günter Scholtysik
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Christopher J. Portier
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Bernhard Walter
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Urs E. Studer
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Hansjörg Danuser
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
  • Article
  • Figures & Data
  • Info & Metrics
  • eLetters
  • PDF
Loading

Abstract

The relaxing property of the K+ channel opener and nitric oxide donor nicorandil and the new K+ channel opener PKF 217-744b was investigated on isolated human ureteral tissue in vitro and in intact ureters of anesthetized pigs in vivo. In addition, nicorandil and its antagonists, glibenclamide and methylene blue, were tested on isolated pig ureter tissue in vitro. Nicorandil decreased the frequency of spontaneous contractions in isolated pig ureter rings. This effect was antagonized by glibenclamide and methylene blue suggesting that the nicorandil induced relaxation of the ureter is mediated by activation of ATP-sensitive K+ channels and involvement of soluble guanylate cyclase. Moreover, nicorandil and PKF 217-744b reduced the amplitude of electrically induced contractions in isolated human ureter rings. Calculations of EC50 values showed that PKF 217-744b [EC50 = 4.83 × 10−8 M] was more potent than nicorandil [EC50 = 4.38 × 10−5 M]. Both drugs reduced the contraction frequency of the pig ureter after intravenous and topical administration in vivo. Intravenous, but not topical, administration of nicorandil and PKF 217-744b significantly decreased arterial blood pressure but did not affect the heart rate. The in vitro findings suggest that K+ channel opening and nitric oxide release mediate the effect of nicorandil. Our in vivo results indicate that PKF 217-744b and nicorandil are promising drugs for clinical application in patients with acute stone colic to relieve obstruction and facilitate stone passage or to relax the ureter before ureteroscopy.

Footnotes

  • This paper was supported by the Swiss National Science Foundation (to H.D., U.E.S., G.S.).

  • Abbreviations:
    KATP channel
    ATP-sensitive K+ channel
    NO
    nitric oxide
    NOS
    NO synthase
    KCa
    calcium-regulated K+ channel
    GC
    guanylate cyclase
    PKF
    PKF 217-744b [(3S,4R)-N-(3.4-dihydro-2.2-dimethyl-3-hydroxy-6-(2-methylpyridin-4-yl)-2H-1-benzopyran)-3-pyridinecarboxy-amid]
    MB
    methylene blue
    • Received November 28, 2001.
    • Accepted April 5, 2002.
  • The American Society for Pharmacology and Experimental Therapeutics
View Full Text

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: 302 (2)
Journal of Pharmacology and Experimental Therapeutics
Vol. 302, Issue 2
1 Aug 2002
  • Table of Contents
  • Index by author
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.
Inhibition of Human and Pig Ureter Motility in Vitro and in Vivo by the K+ Channel Openers PKF 217-744b and Nicorandil
(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 ArticleGASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL

Inhibition of Human and Pig Ureter Motility in Vitro and in Vivo by the K+ Channel Openers PKF 217-744b and Nicorandil

Ruth Weiss, Meike Mevissen, Daniela S. Hauser, Günter Scholtysik, Christopher J. Portier, Bernhard Walter, Urs E. Studer and Hansjörg Danuser
Journal of Pharmacology and Experimental Therapeutics August 1, 2002, 302 (2) 651-658; DOI: https://doi.org/10.1124/jpet.302.2.651

Citation Manager Formats

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

Share
Research ArticleGASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL

Inhibition of Human and Pig Ureter Motility in Vitro and in Vivo by the K+ Channel Openers PKF 217-744b and Nicorandil

Ruth Weiss, Meike Mevissen, Daniela S. Hauser, Günter Scholtysik, Christopher J. Portier, Bernhard Walter, Urs E. Studer and Hansjörg Danuser
Journal of Pharmacology and Experimental Therapeutics August 1, 2002, 302 (2) 651-658; DOI: https://doi.org/10.1124/jpet.302.2.651
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
    • Abstract
    • Materials and Methods
    • Results
    • Discussion
    • Acknowledgments
    • Footnotes
    • References
  • Figures & Data
  • Info & Metrics
  • eLetters
  • PDF

Related Articles

Cited By...

More in this TOC Section

  • Mirabegron Effects in Human Detrusor Tissues
  • Resveratrol Attenuates HFD-Induced Hepatic Lipotoxicity
  • Ligustrazine attenuates liver fibrosis
Show more Gastrointestinal, Hepatic, Pulmonary, and Renal

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