IDEAS home Printed from https://ideas.repec.org/a/nat/nature/v449y2007i7162d10.1038_nature06191.html
   My bibliography  Save this article

Inhibition of nociceptors by TRPV1-mediated entry of impermeant sodium channel blockers

Author

Listed:
  • Alexander M. Binshtok

    (Massachusetts General Hospital and Harvard Medical School, Charlestown, Massachusetts 02129, USA)

  • Bruce P. Bean

    (Harvard Medical School, 220 Longwood Avenue, Boston, Massachusetts 02115, USA)

  • Clifford J. Woolf

    (Massachusetts General Hospital and Harvard Medical School, Charlestown, Massachusetts 02129, USA)

Abstract

Hit where it hurts The snag with most local anaesthetics is their lack of specificity. They are lipophilic, so can enter virtually any neuron, where they indiscriminately block sodium channels in the membrane. A way of blocking the activity of specific pain-sensing neurons without affecting other sensory or motor neurons could be used to create a more targeted form of local anaesthesia, and that is the prospect held out by Binshtok et al. in this issue. They report that the lidocaine derivative QX-314 can be targeted to pain-sensing neurons. Normally QX-314 can't cross the cell membrane. But antipain specificity is ensured by allowing it to enter via the TRPV1 channel, a capsaicin receptor found only in pain-sensing neurons. Co-application of QX-314 and capsaicin in rats blocked mechanical and thermal pain, inducing local anaesthesia, without the paralysis seen in 'normal' lidocaine anaesthesia.

Suggested Citation

  • Alexander M. Binshtok & Bruce P. Bean & Clifford J. Woolf, 2007. "Inhibition of nociceptors by TRPV1-mediated entry of impermeant sodium channel blockers," Nature, Nature, vol. 449(7162), pages 607-610, October.
    • Handle: RePEc:nat:nature:v:449:y:2007:i:7162:d:10.1038_nature06191
    DOI: 10.1038/nature06191
    as

    Download full text from publisher

    File URL: https://www.nature.com/articles/nature06191
    File Function: Abstract
    Download Restriction: Access to the full text of the articles in this series is restricted.
    File URL: https://libkey.io/10.1038/nature06191?utm_source=ideas
    LibKey link: if access is restricted and if your library uses this service, LibKey will redirect you to where you can use your library subscription to access this item
    ---><---

    As the access to this document is restricted, you may want to search for a different version of it.

    Citations

    Citations are extracted by the CitEc Project, subscribe to its RSS feed for this item.
    as


    Cited by:

    1. Zakir, HM & Mostafeezur, RM & Suzuki, A & Hitomi, S & Maeda, T & Seo, K & Yamada, Y & Yamamura, K & Lev, S & Binshtok, AM & Iwata, K & Kitagawa, J, 2012. "Expression of TRPV1 channels after nerve injury provides an essential delivery tool for neuropathic pain attenuation," MPRA Paper 50539, University Library of Munich, Germany.
    2. Hossain Md Zakir & Rahman Md Mostafeezur & Akiko Suzuki & Suzuro Hitomi & Ikuko Suzuki & Takeyasu Maeda & Kenji Seo & Yoshiaki Yamada & Kensuke Yamamura & Shaya Lev & Alexander M Binshtok & Koichi Iwa, 2012. "Expression of TRPV1 Channels after Nerve Injury Provides an Essential Delivery Tool for Neuropathic Pain Attenuation," PLOS ONE, Public Library of Science, vol. 7(9), pages 1-12, September.

    More about this item

    Statistics

    Access and download statistics

    Corrections

    All material on this site has been provided by the respective publishers and authors. You can help correct errors and omissions. When requesting a correction, please mention this item's handle: RePEc:nat:nature:v:449:y:2007:i:7162:d:10.1038_nature06191. See general information about how to correct material in RePEc.

    If you have authored this item and are not yet registered with RePEc, we encourage you to do it here. This allows to link your profile to this item. It also allows you to accept potential citations to this item that we are uncertain about.

    We have no bibliographic references for this item. You can help adding them by using this form .

    If you know of missing items citing this one, you can help us creating those links by adding the relevant references in the same way as above, for each refering item. If you are a registered author of this item, you may also want to check the "citations" tab in your RePEc Author Service profile, as there may be some citations waiting for confirmation.

    For technical questions regarding this item, or to correct its authors, title, abstract, bibliographic or download information, contact: Sonal Shukla or Springer Nature Abstracting and Indexing (email available below). General contact details of provider: http://www.nature.com .

    Please note that corrections may take a couple of weeks to filter through the various RePEc services.

    IDEAS is a RePEc service. RePEc uses bibliographic data supplied by the respective publishers.