Substance P induces inward current and regulates pacemaker currents through tachykinin NK1 receptor in cultured interstitial cells of Cajal of murine small intestine

Eur J Pharmacol. 2004 Jul 8;495(1):35-42. doi: 10.1016/j.ejphar.2004.05.022.

Abstract

We investigated whether substance P modulates pacemaker currents generated in cultured interstitial cells of Cajal of murine small intestine using whole cell patch-clamp techniques at 30 degrees C. Interstitial cells of Cajal generated spontaneous inward currents (pacemaker currents) at a holding potential of -70 mV. Tetrodotoxin, nifedipine, tetraethylammonium, 4-aminopyridine, or glibenclamide did not change the frequency and amplitude of pacemaker currents. However, divalent cations (Ni2+, Mn2+, Cd2+, and Co2+), nonselective cationic channel blockers (gadolinium and flufenamic acid), and a reduction of external Na+ from normal to 1 mM inhibited pacemaker currents indicating that nonselective cation channels are involved in their generation. Substance P depolarized the membrane potential in current clamp mode and produced tonic inward pacemaker currents with reduced frequency and amplitude in voltage clamp mode. [D-Arg1, D-Trp7,9, Leu11] substance P, a tachykinin NK1 receptor antagonist, blocked these substance P-induced responses. Furthermore, [Sar9, Met(O2)11] substance P, a specific tachykinin NK1 receptor agonist, depolarized the membrane and tonic inward currents mimicked those of substance P. Substance P continued to produce tonic inward currents in external Ca2+-free solution or in the presence of chelerythrine, a protein kinase C inhibitor. However, substance P-induced tonic inward currents were blocked by thapsigargin, a Ca2+-ATPase inhibitor in the endoplasmic reticulum or by an external 1 mM Na+ solution. Our results demonstrate that substance P may modulate intestinal motility by acting on the interstitial cells of Cajal by activating nonselective cation channels via the release of intracellular Ca2+ induced by tachykinin NK1 receptor stimulation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 4-Aminopyridine / pharmacology
  • Action Potentials / drug effects
  • Action Potentials / physiology
  • Alkaloids
  • Animals
  • Benzophenanthridines
  • Calcium / metabolism
  • Cations, Divalent / pharmacology
  • Cells, Cultured
  • Electrophysiology / methods
  • Enteric Nervous System / drug effects
  • Enteric Nervous System / physiology
  • Female
  • Glyburide / pharmacology
  • Intestine, Small / drug effects
  • Intestine, Small / innervation*
  • Intestine, Small / pathology*
  • Ion Channels / antagonists & inhibitors
  • Ion Channels / pharmacology
  • Male
  • Membrane Potentials / drug effects*
  • Membrane Potentials / physiology
  • Mice
  • Mice, Inbred BALB C
  • Muscle, Smooth / innervation
  • Neurokinin-1 Receptor Antagonists
  • Nifedipine / pharmacology
  • Phenanthridines / pharmacology
  • Receptors, Neurokinin-1 / physiology*
  • Sinoatrial Node / drug effects
  • Sinoatrial Node / physiology*
  • Sodium / metabolism
  • Substance P / antagonists & inhibitors
  • Substance P / pharmacology*
  • Substance P / physiology
  • Tachykinins / pharmacology
  • Tachykinins / physiology
  • Tetraethylammonium / pharmacology
  • Tetrodotoxin / pharmacology

Substances

  • Alkaloids
  • Benzophenanthridines
  • Cations, Divalent
  • Ion Channels
  • Neurokinin-1 Receptor Antagonists
  • Phenanthridines
  • Receptors, Neurokinin-1
  • Tachykinins
  • Substance P
  • Tetrodotoxin
  • Tetraethylammonium
  • Sodium
  • 4-Aminopyridine
  • chelerythrine
  • Nifedipine
  • Glyburide
  • Calcium