TRPing the switch on pain: an introduction to the chemistry and biology of capsaicin and TRPV1.
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.
Conway
Stuart J
SJ
EaStCHEM, School of Chemistry, Centre for Biomolecular Sciences, University of St Andrews, North Haugh, St Andrews, UK. sjc16@st-andrews.ac.uk
D000818:Animals; D001562:Benzimidazoles / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D002211:Capsaicin / Q000737:chemistry* / Q000378:metabolism*; D006801:Humans; D008024:Ligands; D011759:Pyrrolidines / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D026941:Sodium Channel Blockers / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D050916:TRPV Cation Channels / Q000819:agonists / Q000037:antagonists & inhibitors / Q000737:chemistry* / Q000378:metabolism*; D014508:Urea / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use
D001562:Benzimidazoles; D008024:Ligands; D011759:Pyrrolidines; C512301:SB 705498; D026941:Sodium Channel Blockers; D050916:TRPV Cation Channels; D014508:Urea; C031000:benzimidazole; D002211:Capsaicin