Intracolonical administration of protease-activated receptor-2 agonists produced visceral hyperalgesia by up-regulating serotonin in the colon of rats

Eur J Pharmacol. 2009 Mar 15;606(1-3):199-204. doi: 10.1016/j.ejphar.2009.01.031. Epub 2009 Jan 30.

Abstract

This study aimed to investigate the underlying mechanism of protease-activated receptor-2 (PAR-2) agonist-induced visceral hyperalgesia. Male Sprague-Dawley rat pups were submitted to colonic injection of PAR-2 agonist for 6 consecutive days. The visceral sensitivity to colorectal distention was evaluated by electromyography. The enterochromaffin (EC) cell number, 5-HT content and tryrptophan hydroxylase (TPH) protein expression were detected with immunohistochemistry, fluorescent measurement and Western blot analysis. PAR-2 agonist induced a significant increase of visceral nociceptive response to colorectal distention and a series of neurochemical changes in rat colon, including proliferation of EC cells, increased 5-HT content and enhanced TPH expression. Expression of PAR-2 in EC cells was reported for the first time. Further, selective 5-HT(3) receptor antagonist alosteron significantly inhibited PAR-2-induced visceral hyperalgesia. The enhanced 5-HT signaling is likely responsible for the visceral hyperalgesia induced by PAR-2 agonist. Interruption of this pathway is a possible target for the treatment of visceral hyperalgesia in gastrointestinal diseases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Carbolines / pharmacology
  • Cell Count
  • Colon / drug effects*
  • Colon / metabolism
  • Colon / pathology
  • Enterochromaffin Cells / drug effects
  • Enterochromaffin Cells / metabolism
  • Enterochromaffin Cells / pathology
  • Hyperalgesia / chemically induced*
  • Hyperalgesia / metabolism
  • Hyperalgesia / therapy
  • Male
  • Oligopeptides / administration & dosage
  • Oligopeptides / adverse effects*
  • Oligopeptides / chemistry
  • Oligopeptides / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Receptor, PAR-2 / agonists*
  • Receptor, PAR-2 / metabolism
  • Serotonin / metabolism*
  • Tryptophan Hydroxylase / metabolism
  • Up-Regulation / drug effects*

Substances

  • Carbolines
  • Oligopeptides
  • Receptor, PAR-2
  • alosetron
  • Serotonin
  • Tryptophan Hydroxylase