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The role of endogenous molecules in modulating pain through transient receptor potential vanilloid 1 (TRPV1).

Publication ,  Journal Article
Morales-Lázaro, SL; Simon, SA; Rosenbaum, T
Published in: J Physiol
July 1, 2013

Pain is a physiological response to a noxious stimulus that decreases the quality of life of those sufferring from it. Research aimed at finding new therapeutic targets for the treatment of several maladies, including pain, has led to the discovery of numerous molecular regulators of ion channels in primary afferent nociceptive neurons. Among these receptors is TRPV1 (transient receptor potential vanilloid 1), a member of the TRP family of ion channels. TRPV1 is a calcium-permeable channel, which is activated or modulated by diverse exogenous noxious stimuli such as high temperatures, changes in pH, and irritant and pungent compounds, and by selected molecules released during tissue damage and inflammatory processes. During the last decade the number of endogenous regulators of TRPV1's activity has increased to include lipids that can negatively regulate TRPV1, as is the case for cholesterol and PIP2 (phosphatidylinositol 4,5-biphosphate) while, in contrast, other lipids produced in response to tissue injury and ischaemic processes are known to positively regulate TRPV1. Among the latter, lysophosphatidic acid activates TRPV1 while amines such as N-acyl-ethanolamines and N-acyl-dopamines can sensitize or directly activate TRPV1. It has also been found that nucleotides such as ATP act as mediators of chemically induced nociception and pain and gases, such as hydrogen sulphide and nitric oxide, lead to TRPV1 activation. Finally, the products of lipoxygenases and omega-3 fatty acids among other molecules, such as divalent cations, have also been shown to endogenously regulate TRPV1 activity. Here we provide a comprehensive review of endogenous small molecules that regulate the function of TRPV1. Acting through mechanisms that lead to sensitization and desensitization of TRPV1, these molecules regulate pathways involved in pain and nociception. Understanding how these compounds modify TRPV1 activity will allow us to comprehend how some pathologies are associated with its deregulation.

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Published In

J Physiol

DOI

EISSN

1469-7793

Publication Date

July 1, 2013

Volume

591

Issue

13

Start / End Page

3109 / 3121

Location

England

Related Subject Headings

  • TRPV Cation Channels
  • Physiology
  • Pain
  • Humans
  • Animals
  • 42 Health sciences
  • 32 Biomedical and clinical sciences
  • 31 Biological sciences
  • 11 Medical and Health Sciences
  • 06 Biological Sciences
 

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Morales-Lázaro, S. L., Simon, S. A., & Rosenbaum, T. (2013). The role of endogenous molecules in modulating pain through transient receptor potential vanilloid 1 (TRPV1). J Physiol, 591(13), 3109–3121. https://doi.org/10.1113/jphysiol.2013.251751
Morales-Lázaro, Sara L., Sidney A. Simon, and Tamara Rosenbaum. “The role of endogenous molecules in modulating pain through transient receptor potential vanilloid 1 (TRPV1).J Physiol 591, no. 13 (July 1, 2013): 3109–21. https://doi.org/10.1113/jphysiol.2013.251751.
Morales-Lázaro SL, Simon SA, Rosenbaum T. The role of endogenous molecules in modulating pain through transient receptor potential vanilloid 1 (TRPV1). J Physiol. 2013 Jul 1;591(13):3109–21.
Morales-Lázaro, Sara L., et al. “The role of endogenous molecules in modulating pain through transient receptor potential vanilloid 1 (TRPV1).J Physiol, vol. 591, no. 13, July 2013, pp. 3109–21. Pubmed, doi:10.1113/jphysiol.2013.251751.
Morales-Lázaro SL, Simon SA, Rosenbaum T. The role of endogenous molecules in modulating pain through transient receptor potential vanilloid 1 (TRPV1). J Physiol. 2013 Jul 1;591(13):3109–3121.
Journal cover image

Published In

J Physiol

DOI

EISSN

1469-7793

Publication Date

July 1, 2013

Volume

591

Issue

13

Start / End Page

3109 / 3121

Location

England

Related Subject Headings

  • TRPV Cation Channels
  • Physiology
  • Pain
  • Humans
  • Animals
  • 42 Health sciences
  • 32 Biomedical and clinical sciences
  • 31 Biological sciences
  • 11 Medical and Health Sciences
  • 06 Biological Sciences