TRPV1 Activation by Anandamide via a Unique Lipid Pathway

J Chem Inf Model. 2021 Dec 27;61(12):5742-5746. doi: 10.1021/acs.jcim.1c00893. Epub 2021 Nov 15.

Abstract

The capsaicin receptor, transient receptor potential vanilloid type 1 (TRPV1), is a polymodal channel that has been implicated in the perception of pain and can be modulated by a variety of cannabinoid ligands. Here we report TRPV1 channel activation by the endocannabinoid, anandamide (AEA), in a unique, peripheral binding site via extended MD simulations. These results aim to expand the understanding of TRPV1 and assist in the development of new TRPV1 modulators.

Publication types

  • Letter
  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Arachidonic Acids / pharmacology
  • Cannabinoid Receptor Modulators* / metabolism
  • Endocannabinoids*
  • Polyunsaturated Alkamides / pharmacology
  • Receptor, Cannabinoid, CB1 / metabolism
  • TRPV Cation Channels

Substances

  • Arachidonic Acids
  • Cannabinoid Receptor Modulators
  • Endocannabinoids
  • Polyunsaturated Alkamides
  • Receptor, Cannabinoid, CB1
  • TRPV Cation Channels
  • anandamide