Inhibition of gastric acid secretion by oxyntomodulin and its 19-37 fragment in the conscious rat

Am J Physiol. 1993 May;264(5 Pt 1):G816-23. doi: 10.1152/ajpgi.1993.264.5.G816.

Abstract

Oxyntomodulin (Oxm) is a hormone, released from the intestine during digestion. Its target tissue is the gastric mucosa, where it inhibits acid secretion. It contains the 29-amino acid glucagon moiety, extended at its COOH-terminal end by an octapeptide. The glucagon moiety contains a basic doublet (Arg17-Arg18). Our working hypothesis was that the mode of action of Oxm may imply a processing of the molecule at the Arg-Arg doublet, releasing Oxm-(19-37). We compared the effect of Oxm with that of Oxm-(19-37) on gastric acid secretion in the conscious rat provided with a chronic gastric fistula. The acid secretion was plateau stimulated by a perfusion of either pentagastrin or histamine. Whereas Oxm or Oxm-(19-37) had no effect on basal acid secretion, both peptides inhibited pentagastrin (0.5 micrograms.kg-1.h-1)- and histamine (0.4 mg.kg-1.h-1)-stimulated acid secretion in a dose-dependent manner. When the metabolic clearance rate for each peptide was taken into account, the 19-37 fragment was as potent as the whole Oxm, regardless of the type of stimulant. When the dose of pentagastrin was increased from 0.175 to 1.1 micrograms.kg-1.h-1, the extent of inhibition induced by Oxm (40 pmol/kg) also increased. In contrast, when the dose of histamine was increased from 0.25 to 1.2 mg.kg-1.h-1, the extent of inhibition induced by Oxm (40 pmol/kg) decreased. Oxm-(19-37) (70-140 pmol/kg) displayed the same behavior as the whole molecule under both types of stimulation.(ABSTRACT TRUNCATED AT 250 WORDS)

Publication types

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

MeSH terms

  • Animals
  • Cell Membrane / metabolism
  • Dose-Response Relationship, Drug
  • Gastric Acid / metabolism*
  • Gastric Mucosa / drug effects
  • Glucagon-Like Peptides / metabolism
  • Glucagon-Like Peptides / pharmacology*
  • Histamine / pharmacology
  • Kinetics
  • Liver / metabolism
  • Male
  • Oxyntomodulin
  • Pentagastrin / pharmacology
  • Peptide Fragments / pharmacology*
  • Rats
  • Rats, Wistar
  • Time Factors

Substances

  • Oxyntomodulin
  • Peptide Fragments
  • oxyntomodulin (19-37)
  • Glucagon-Like Peptides
  • Histamine
  • Pentagastrin