TRPing the switch on pain: an introduction to the chemistry and biology of capsaicin and TRPV1

Chem Soc Rev. 2008 Aug;37(8):1530-45. doi: 10.1039/b610226n. Epub 2008 Jun 20.

Abstract

Capsaicin has elicited great interest for many centuries due to its noticeable culinary and medical properties. The discovery of its receptor, TRPV1, sparked an explosion of interest in TRPV1 and the development of TRPV1 agonists and antagonists. This tutorial review provides an introduction to the history of both capsaicin and TRPV1. Two TRPV1 antagonists that are undergoing clinical trials are highlighted, as are some light-activated molecular tools that are enabling the intracellular study of this protein. This article will be of interest to chemists and biologists with an interest in TRPV1, cell signalling, or medicinal and biological chemistry.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Benzimidazoles / chemistry
  • Benzimidazoles / pharmacology
  • Benzimidazoles / therapeutic use
  • Capsaicin / chemistry*
  • Capsaicin / metabolism*
  • Humans
  • Ligands
  • Pyrrolidines / chemistry
  • Pyrrolidines / pharmacology
  • Pyrrolidines / therapeutic use
  • Sodium Channel Blockers / chemistry
  • Sodium Channel Blockers / pharmacology
  • Sodium Channel Blockers / therapeutic use
  • TRPV Cation Channels / agonists
  • TRPV Cation Channels / antagonists & inhibitors
  • TRPV Cation Channels / chemistry*
  • TRPV Cation Channels / metabolism*
  • Urea / analogs & derivatives
  • Urea / chemistry
  • Urea / pharmacology
  • Urea / therapeutic use

Substances

  • Benzimidazoles
  • Ligands
  • Pyrrolidines
  • SB 705498
  • Sodium Channel Blockers
  • TRPV Cation Channels
  • Urea
  • benzimidazole
  • Capsaicin