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Oxyntomodulin and its (19-37) and (30-37) fragments inhibit histamine-stimulated gastric acid secretion in the conscious rat.

Abstract：

:Oxyntomodulin, a hormone released from jejuno-ileum and composed of the glucagon sequence extended by a C-terminal octapeptide displays original tissue specificity for the gastric mucosa. The aim of this study was to compare the effect of oxyntomodulin on histamine (0.4 mg/kg per h)-stimulated gastric acid secretion in the conscious rat to that of three of its fragments: oxyntomodulin-(19-37) produced from oxyntomodulin by enzymatic cleavage, oxyntomodulin-(30-37) corresponding to the molecular difference between oxyntomodulin and glucagon and oxyntomodulin-(32-37) produced during proglucagon processing to glucagon. The metabolic clearance rate (MCR) in the anesthetized rat was evaluated for each peptide. Oxyntomodulin, oxyntomodulin-(19-37) and oxyntomodulin-(30-37) inhibited the histamine-stimulated gastric acid secretion dose dependently. The dose-response curves for oxyntomodulin and oxyntomodulin-(19-37) were parallel. The potency of oxyntomodulin (19-37) (ED50 approximately 70 pmol/kg) was the same as that of oxyntomodulin (ED50 approximately 35 nmol/kg) after correction of the curve for the MCR (two-fold higher for the fragment). Although the dose-response curve for oxyntomodulin-(30-37) was not entirely parallel to that of the two other peptides, its maximal inhibition (at 15 nmol/kg) was the same as that of oxyntomodulin-(19-37). Thus, oxyntomodulin-(30-37) was an efficient as the longer molecules but approximately 150-fold less potent than oxyntomodulin. The MCR for oxyntomodulin-(30-37) was approximately 250 fold higher than that of oxyntomodulin, partly explaining the difference in potency. The (32-37) fragment, which is naturally released from the endocrine pancreas, was devoid of activity.(ABSTRACT TRUNCATED AT 250 WORDS)

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Carles-Bonnet C,Jarrousse C,Niel H,Martinez J,Bataille D

doi

10.1016/0014-2999(91)90720-b

subject

Has Abstract

pub_date

1991-10-15 00:00:00

pages

245-52

issue

eissn

0014-2999

issn

1879-0712

pii

0014-2999(91)90720-B

journal_volume

203

pub_type

杂志文章

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Oxyntomodulin and its (19-37) and (30-37) fragments inhibit histamine-stimulated gastric acid secretion in the conscious rat.