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

Agonist-Dependent Potentiation of Vanilloid Receptor Transient Receptor Potential Vanilloid Type 1 Function by Stilbene Derivatives

Xuan Zhang, Xiao-Na Du, Guo-Hong Zhang, Zhan-Feng Jia, Xing-Juan Chen, Dong-Yang Huang, Bo-Yi Liu and Hai-Lin Zhang
Molecular Pharmacology May 2012, 81 (5) 689-700; DOI: https://doi.org/10.1124/mol.111.076000
Xuan Zhang
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Xiao-Na Du
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Guo-Hong Zhang
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Zhan-Feng Jia
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Xing-Juan Chen
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Dong-Yang Huang
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Bo-Yi Liu
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Hai-Lin Zhang
  • 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

Transient receptor potential vanilloid type 1 (TRPV1) is a nonselective cation channel activated by capsaicin, low pH, and noxious heat and plays a key role in nociception. Understanding mechanisms for functional modulation of TRPV1 has important implications. One characteristic of TRPV1 is that channel activity induced by either capsaicin or other activators can be sensitized or modulated by factors involving different cell signaling mechanisms. In this study, we describe a novel mechanism for the modulation of TRPV1 function: TRPV1 function is modulated by 4,4′-diisothiocyanatostilbene-2,2′-disulfonic acid (DIDS) and its analogs. We found that, in rat dorsal root ganglion neurons, although DIDS did not induce the activation of TRPV1 per se but drastically increased the TRPV1 currents induced by either capsaicin or low pH. DIDS also blocked the tachyphylaxis of the low pH-induced TRPV1 currents. 4-Acetamido-4′-isothiocyanatostilbene-2,2′-disulfonic acid (SITS), a DIDS analog, failed to enhance the capsaicin-evoked TRPV1 current but increased the low pH-evoked TRPV1 currents, with an effect comparable with that of DIDS. SITS also blocked the low pH-induced tachyphylaxis. DIDS also potentiated the currents of TRPV1 channels expressed in human embryonic kidney 293 cells, with an effect of left-shifting the concentration-response curve of the capsaicin-induced TRPV1 currents. This study demonstrates that DIDS and SITS, traditionally used chloride channel blockers, can modify TRPV1 channel function in an agonist-dependent manner. The results provide new input for understanding TRPV1 modulation and developing new modulators of TRPV1 function.

Footnotes

  • ↵Embedded Image The online version of this article (available at http://molpharm.aspetjournals.org) contains supplemental material.

  • This work was supported by the National Natural Science Foundation of China [Grant 30730031] (to H.-L.Z.); and the National Basic Research Program [Grant 2007CB512100].

  • Article, publication date, and citation information can be found at http://molpharm.aspetjournals.org.

    http://dx.doi.org/10.1124/mol.111.076000.

  • ABBREVIATIONS:

    TRPV1
    transient receptor potential vanilloid type 1
    AEA
    anandamide/arachidonylethanolamide
    ASIC
    acid-sensing ion channel
    CAP
    capsaicin
    DADS
    4,4′-diaminostilbene-2,2′-disulfonic acid
    DIDS
    4,4′-diisothiocyanatostilbene-2,2′-disulfonic acid
    DMEM
    Dulbecco's modified Eagle's medium
    DNDS
    4,4-dinitro-2,2-stilbenedisulfonic acid
    DRG
    dorsal root ganglion
    HEK
    human embryonic kidney
    PIP2
    phosphatidylinositol bisphosphate
    PKC
    protein kinase C
    RR
    ruthenium red
    SITS
    4-acetamido-4′-isothiocyanatostilbene-2,2′-disulfonic acid
    TM
    transmembrane.

  • Received October 12, 2011.
  • Accepted February 7, 2012.
  • Copyright © 2012 The American Society for Pharmacology and Experimental Therapeutics
View Full Text

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: 81 (5)
Molecular Pharmacology
Vol. 81, Issue 5
1 May 2012
  • Table of Contents
  • Table of Contents (PDF)
  • About the Cover
  • Index by author
  • Editorial Board (PDF)
  • Front Matter (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.
Agonist-Dependent Potentiation of Vanilloid Receptor Transient Receptor Potential Vanilloid Type 1 Function by Stilbene Derivatives
(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

Potentiation of TRPV1 by DIDS

Xuan Zhang, Xiao-Na Du, Guo-Hong Zhang, Zhan-Feng Jia, Xing-Juan Chen, Dong-Yang Huang, Bo-Yi Liu and Hai-Lin Zhang
Molecular Pharmacology May 1, 2012, 81 (5) 689-700; DOI: https://doi.org/10.1124/mol.111.076000

Citation Manager Formats

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

Share
Research ArticleArticle

Potentiation of TRPV1 by DIDS

Xuan Zhang, Xiao-Na Du, Guo-Hong Zhang, Zhan-Feng Jia, Xing-Juan Chen, Dong-Yang Huang, Bo-Yi Liu and Hai-Lin Zhang
Molecular Pharmacology May 1, 2012, 81 (5) 689-700; DOI: https://doi.org/10.1124/mol.111.076000
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
    • Introduction
    • Materials and Methods
    • Results
    • Discussion
    • Authorship Contributions
    • Acknowledgments
    • Footnotes
    • References
  • Figures & Data
  • Info & Metrics
  • eLetters
  • PDF

Related Articles

Cited By...

More in this TOC Section

  • Therapeutic Effects of FGF23 Antagonists in Hyp Mice
  • TRPV3 and TRPV4 Channels Coassemble into Heterotetramers
  • Secretin Amino-Terminal Structure-Activity Relationships and Complementary Mutagenesis at the Site of Docking to the Secretin Receptor
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 © 2022 by the American Society for Pharmacology and Experimental Therapeutics