TRPV1 (vanilloid receptor) in the urinary tract: expression, function and clinical applications

Naunyn Schmiedebergs Arch Pharmacol. 2006 Jul;373(4):287-99. doi: 10.1007/s00210-006-0073-2. Epub 2006 May 24.

Abstract

The transient receptor potential vanilloid subfamily 1 (TRPV1) is an ion channel activated by capsaicin, heat, protons and endogenous ligands such as anandamide. It is largely expressed in the urinary tract of mammals. Structures in which the receptor expression is firmly established include sensory fibers and urothelial cells, although the presence of TRPV1 in other cell types has been reported. As in other systems, pain perception was the first role attributed to TRPV1 in the urinary tract. However, it is now increasingly clear that TRPV1 also regulates the frequency of bladder reflex contractions, either through direct excitation of sensory fibers or through urothelial-sensory fiber cross talk involving the release of neuromediators from the epithelial cells. In addition, the recent identification of the receptor in urothelial and prostatic cancer cells raise the exciting hypothesis that TRPV1 is involved in cell differentiation. Desensitization of the receptor by capsaicin and resiniferatoxin has been investigated for therapeutic purposes. For the moment, lower urinary tract dysfunctions in which some benefit was obtained include painful bladder syndrome and overactive bladder of neurogenic and non-neurogenic origin. However, desensitization may become obsolete when non-toxic, potent TRPV1 antagonists become available.

Publication types

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

MeSH terms

  • Animals
  • Arachidonic Acids / metabolism
  • Capsaicin / pharmacology
  • Clinical Trials as Topic
  • Cystitis / metabolism
  • Diterpenes / pharmacology
  • Endocannabinoids
  • Humans
  • Neurons, Afferent / metabolism
  • Polyunsaturated Alkamides
  • TRPV Cation Channels / agonists
  • TRPV Cation Channels / metabolism*
  • Urinary Tract / metabolism*
  • Urothelium / cytology
  • Urothelium / metabolism

Substances

  • Arachidonic Acids
  • Diterpenes
  • Endocannabinoids
  • Polyunsaturated Alkamides
  • TRPV Cation Channels
  • TRPV1 receptor
  • resiniferatoxin
  • Capsaicin
  • anandamide