Silencing of vanilloid receptor TRPV1 by RNAi reduces neuropathic and visceral pain in vivo

Biochem Biophys Res Commun. 2006 Nov 10;350(1):238-43. doi: 10.1016/j.bbrc.2006.09.037. Epub 2006 Sep 18.

Abstract

RNA interference (RNAi) has proven to be a powerful technique to study the function of genes by producing knock-down phenotypes. Here, we report that intrathecal injection of an siRNA against the transient receptor potential vanilloid receptor 1 (TRPV1) reduced cold allodynia of mononeuropathic rats by more than 50% over a time period of approximately 5 days. A second siRNA targeted to a different region of the TRPV1 gene was employed and confirmed the analgesic action of a TRPV1 knock-down. Furthermore, siRNA treatment diminished spontaneous visceral pain behavior induced by capsaicin application to the rectum of mice. The analgesic effect of siRNA-mediated knockdown of TRPV1 in the visceral pain model was comparable to that of the low-molecular weight receptor antagonist BCTC. Our data demonstrate that TRPV1 antagonists, including TRPV1 siRNAs, have potential in the treatment of both, neuropathic and visceral pain.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Base Sequence
  • COS Cells
  • Capsaicin / pharmacology
  • Chlorocebus aethiops
  • Colitis / chemically induced
  • Colitis / genetics
  • Colitis / metabolism
  • Colitis / pathology
  • Disease Models, Animal
  • Humans
  • Male
  • Mice
  • Molecular Sequence Data
  • Nervous System Diseases / genetics
  • Nervous System Diseases / metabolism*
  • Nervous System Diseases / pathology*
  • Pain / genetics
  • Pain / metabolism*
  • Pain / pathology*
  • Pyrazines / pharmacology
  • Pyridines / pharmacology
  • RNA Interference*
  • Rats
  • Sequence Alignment
  • Sequence Homology, Amino Acid
  • TRPV Cation Channels / antagonists & inhibitors
  • TRPV Cation Channels / genetics
  • TRPV Cation Channels / metabolism*

Substances

  • N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2H)-carboxamide
  • Pyrazines
  • Pyridines
  • TRPV Cation Channels
  • Capsaicin