Combined blockade of 5-HT3- and 5-HT4-serotonin receptors inhibits colonic functions in conscious rats and mice

J Pharmacol Exp Ther. 1997 Apr;281(1):284-90.

Abstract

We have already reported that 5-hydroxytryptamine3 (5-HT3) receptor antagonists failed to modify 5-HT-accelerated colonic transit in conscious rats, but the 5-HT3 and 5-HT4 receptor dual antagonist FK1052 prevented the enhancement. In this study, the inhibitory effect on the stimulated colonic transit was not also observed with 5-HT4 receptor antagonists (SDZ205-557 and SB204070) in freely moving rats with chronic cannulas implanted into the proximal colon. In contrast, combined antagonism by simultaneous administration of ondansetron and the 5-HT4 receptor antagonist exerted a drastic inhibitory effect on the propulsive motility. Furthermore, we examined the effect of 5-HT receptor antagonists on 5-HT-induced fluid secretion in mice. Although none of these selective 5-HT receptor antagonists (YM060 and ondansetron as 5-HT3 receptor antagonist, SB204070 as 5-HT4 receptor antagonist) by itself produced a great inhibition of the 5-HT-induced diarrhea, the combination of a 5-HT3 receptor antagonist and a 5-HT4 receptor antagonist markedly reduced the diarrhea. These data suggest that 5-HT-accelerated colonic motility and 5-HT-evoked fluid secretion are mediated by both 5-HT3 and 5-HT4 receptors and that the pathways activated by these receptors may collaborate.

MeSH terms

  • 4-Aminobenzoic Acid / pharmacology
  • Animals
  • Colon / drug effects*
  • Colon / physiology
  • Dioxanes / pharmacology
  • Male
  • Mice
  • Ondansetron / pharmacology
  • Piperidines / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Serotonin / physiology*
  • Receptors, Serotonin, 5-HT3
  • Receptors, Serotonin, 5-HT4
  • Serotonin Antagonists / pharmacology*
  • para-Aminobenzoates

Substances

  • Dioxanes
  • Piperidines
  • Receptors, Serotonin
  • Receptors, Serotonin, 5-HT3
  • Serotonin Antagonists
  • para-Aminobenzoates
  • 2-methoxy-4-amino-5-chlorobenzoic acid 2-(diethylamino)ethyl ester
  • SB 204070A
  • Receptors, Serotonin, 5-HT4
  • Ondansetron
  • 4-Aminobenzoic Acid