Modulation of capsaicin-evoked visceral pain and referred hyperalgesia by protease-activated receptors 1 and 2

J Pharmacol Sci. 2004 Mar;94(3):277-85. doi: 10.1254/jphs.94.277.

Abstract

Protease-activated receptors (PARs) 1 and 2 are expressed in capsaicin-sensitive sensory neurons, being anti- and pro-nociceptive, respectively. Given the possible cross talk between PAR-2 and capsaicin receptors, we investigated if PAR-2 activation could facilitate capsaicin-evoked visceral pain and referred hyperalgesia in the mouse and also examined the effect of PAR-1 activation in this model. Intracolonic (i.col.) administration of capsaicin triggered visceral pain-related nociceptive behavior, followed by referred hyperalgesia. The capsaicin-evoked visceral nociception was suppressed by intraperitoneal (i.p.) TFLLR-NH2, a PAR-1-activating peptide, but not FTLLR-NH2, a control peptide, and unaffected by i.col. TFLLR-NH2. SLIGRL-NH2, a PAR-2-activating peptide, but not LRGILS-NH2, a control peptide, administered i.col., facilitated the capsaicin-evoked visceral nociception 6-18 h after administration, while i.p. SLIGRL-NH2 had no effect. The capsaicin-evoked referred hyperalgesia was augmented by i.col. SLIGRL-NH2, but not LRGILS-NH2, 6-18 h after administration, and unaffected by i.p. SLIGRL-NH2, and i.p. or i.col. TFLLR-NH2. Our data suggest that PAR-1 is antinociceptive in processing of visceral pain, whereas PAR-2 expressed in the colonic luminal surface, upon activation, produces delayed sensitization of capsaicin receptors, resulting in facilitation of visceral pain and referred hyperalgesia.

Publication types

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

MeSH terms

  • Administration, Rectal
  • Animals
  • Behavior, Animal / drug effects
  • Capsaicin / administration & dosage
  • Capsaicin / adverse effects*
  • Capsaicin / antagonists & inhibitors
  • Colon / drug effects
  • Colon / innervation
  • Dose-Response Relationship, Drug
  • Drug Synergism
  • Drug Therapy, Combination
  • Hyperalgesia / chemically induced*
  • Hyperalgesia / complications
  • Hyperalgesia / physiopathology
  • Injections, Intraperitoneal
  • Male
  • Mice
  • Oligopeptides / administration & dosage
  • Oligopeptides / chemistry
  • Oligopeptides / pharmacokinetics
  • Pain / chemically induced*
  • Pain / complications
  • Pain / physiopathology
  • Pain Measurement / methods
  • Peptides / administration & dosage
  • Peptides / pharmacokinetics
  • Receptor, PAR-1 / drug effects
  • Receptor, PAR-1 / genetics
  • Receptor, PAR-1 / metabolism*
  • Receptor, PAR-2 / drug effects
  • Receptor, PAR-2 / genetics
  • Receptor, PAR-2 / metabolism*
  • Time Factors
  • Up-Regulation
  • Viscera / drug effects*
  • Viscera / innervation
  • Viscera / physiopathology

Substances

  • Oligopeptides
  • PAR-1-activating peptide
  • Peptides
  • Receptor, PAR-1
  • Receptor, PAR-2
  • leucyl-arginyl-glycyl-isoleucyl-leucyl-serinamide
  • phenylalanyl-threonyl-leucyl-leucyl-argininamide
  • seryl-leucyl-isoleucyl-glycyl--arginyl-leucinamide
  • seryl-leucyl-isoleucyl-glycyl-arginyl-leucine
  • amastatin
  • Capsaicin