Agonists of proteinase-activated receptor 2 excite guinea pig ileal myenteric neurons

Eur J Pharmacol. 2001 Nov 23;431(3):311-4. doi: 10.1016/s0014-2999(01)01447-9.

Abstract

The effects of proteinase-activated receptor 2 (PAR2) agonists on the electrical properties of intact guinea pig ileal myenteric neurons were measured with intracellular microelectrodes. Approximately 52% of AH neurons and 41% of S neurons responded to pressure ejection of SLIGRL-NH(2) or trypsin with a prolonged depolarization that was often accompanied by increased excitability. When added to the bathing solution, trypsin caused a concentration-dependent depolarization of responding neurons with an estimated EC(50) value of 87 nM. Collectively, these novel observations indicate that PAR2 excites a proportion of myenteric neurons, which may contribute to dysmotility during intestinal inflammation.

Publication types

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

MeSH terms

  • Animals
  • Gastrointestinal Motility
  • Guinea Pigs
  • Ileum / drug effects*
  • Ileum / innervation
  • In Vitro Techniques
  • Membrane Potentials
  • Microelectrodes
  • Myenteric Plexus / physiology
  • Neurons / drug effects
  • Neurons / physiology
  • Oligopeptides / pharmacology
  • Receptor, PAR-2
  • Receptors, Thrombin / agonists*
  • Trypsin / pharmacology

Substances

  • Oligopeptides
  • Receptor, PAR-2
  • Receptors, Thrombin
  • seryl-leucyl-isoleucyl-glycyl--arginyl-leucinamide
  • Trypsin