Activation of submucosal 5-HT(3) receptors elicits a somatostatin-dependent inhibition of ion secretion in rat colon

Br J Pharmacol. 2010 Apr;159(8):1623-5. doi: 10.1111/j.1476-5381.2010.00653.x. Epub 2010 Mar 5.

Abstract

Background and purpose: 5-Hydroxytryptamine (5-HT) is a key regulator of the gastrointestinal system and we have shown that submucosal neuronal 5-HT(3) receptors exerted a novel inhibitory effect on colonic ion transport. The aim of the present study was to investigate the precise mechanism(s) underlying this inhibitory effect.

Experimental approach: Mucosa/submucosa or mucosa-only preparations from rat distal colon were mounted in Ussing chambers for measurement of short-circuit current (I(sc)) as an indicator of ion secretion. Somatostatin release was determined with radioimmunoassay. Intracellular cAMP content was measured with enzyme-linked immunoadsorbent assay (elisa). Immunohistochemical techniques were used to study the expression of 5-HT(3) receptors, somatostatin and somatostatin receptors in colonic tissue.

Key results: In rat distal colonic mucosa/submucosa preparations, pretreatment with 5-HT(3) receptor antagonists enhanced 5-HT-induced increases in I(sc). However, in mucosa-only preparations without retained neural elements, pretreatment with 5-HT(3) receptor antagonists inhibited 5-HT-induced DeltaI(sc). Pretreatment with a somatostatin-2 (sst(2)) receptor antagonist in mucosa/submucosa preparations augmented 5-HT-induced DeltaI(sc). Combination of sst(2) and 5-HT(3) receptor antagonists did not cause further enhancement of 5-HT-induced DeltaI(sc). Moreover, both sst(2) and 5-HT(3) receptor antagonists enhanced 5-HT-induced increase in intracellular cAMP concentration in the mucosa/submucosa preparations. 5-HT released somatostatin from rat colonic mucosa/submucosa preparations, an effect prevented by pretreatment with 5-HT(3) receptor antagonists. Immunohistochemical staining demonstrated the presence of 5-HT(3) receptors on submucosal somatostatin neurons and of sst(2) receptors on colonic mucosa.

Conclusion and implications: Activation of neuronal 5-HT(3) receptors in the submucosal plexus of rat colon suppressed 5-HT-induced ion secretion by releasing somatostatin from submucosal neurons.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Colon / drug effects*
  • Colon / metabolism
  • Cyclic AMP / metabolism
  • Fluorescent Antibody Technique
  • Intestinal Mucosa / drug effects*
  • Intestinal Mucosa / metabolism
  • Ions
  • Male
  • Molecular Sequence Data
  • Oligopeptides / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Serotonin, 5-HT3 / chemistry
  • Serotonin 5-HT3 Receptor Agonists*
  • Serotonin 5-HT3 Receptor Antagonists
  • Serotonin Antagonists / pharmacology
  • Somatostatin / physiology*
  • Tetrodotoxin / pharmacology

Substances

  • CYN 154806
  • Ions
  • Oligopeptides
  • Receptors, Serotonin, 5-HT3
  • Serotonin 5-HT3 Receptor Agonists
  • Serotonin 5-HT3 Receptor Antagonists
  • Serotonin Antagonists
  • Tetrodotoxin
  • Somatostatin
  • Cyclic AMP