Inhibition of TRPV1 channels by a naturally occurring omega-9 fatty acid reduces pain and itch.

Journal Article (Journal Article)

The transient receptor potential vanilloid 1 (TRPV1) ion channel is mainly found in primary nociceptive afferents whose activity has been linked to pathophysiological conditions including pain, itch and inflammation. Consequently, it is important to identify naturally occurring antagonists of this channel. Here we show that a naturally occurring monounsaturated fatty acid, oleic acid, inhibits TRPV1 activity, and also pain and itch responses in mice by interacting with the vanilloid (capsaicin)-binding pocket and promoting the stabilization of a closed state conformation. Moreover, we report an itch-inducing molecule, cyclic phosphatidic acid, that activates TRPV1 and whose pruritic activity, as well as that of histamine, occurs through the activation of this ion channel. These findings provide insights into the molecular basis of oleic acid inhibition of TRPV1 and also into a way of reducing the pathophysiological effects resulting from its activation.

Full Text

Duke Authors

Cited Authors

  • Morales-Lázaro, SL; Llorente, I; Sierra-Ramírez, F; López-Romero, AE; Ortíz-Rentería, M; Serrano-Flores, B; Simon, SA; Islas, LD; Rosenbaum, T

Published Date

  • October 10, 2016

Published In

Volume / Issue

  • 7 /

Start / End Page

  • 13092 -

PubMed ID

  • 27721373

Pubmed Central ID

  • PMC5062500

Electronic International Standard Serial Number (EISSN)

  • 2041-1723

Digital Object Identifier (DOI)

  • 10.1038/ncomms13092


  • eng

Conference Location

  • England