Evaluation of biologic gastrin activity of compound CI-988 in the isolated, vascularly perfused rat stomach.

Abstract:

BACKGROUND:The peptoid CI-988 has previously been shown to have high affinity for the cholecystokinin (CCK)-B/gastrin receptor and has been reported to be a powerful CCK antagonist in many systems, although it has agonist activity on histidine decarboxylase in the rat. METHODS:In the present study the effect of CI-988 on acid secretion and histamine release in the totally isolated, vascularly perfused rat stomach was assessed. RESULTS:CI-988 was found to be a gastrin agonist with regard to the stimulation of both histamine release and acid secretion. CONCLUSION:Thus, in this stomach model CI-988 behaved as a CCKB/gastrin agonist. The present study underlines the importance of testing the biologic activity of ligands in models with sufficient sensitivity.

journal_name

Scand J Gastroenterol

authors

Marvik R,Sandvik AK,Waldum HL

doi

10.3109/00365529709025092

subject

Has Abstract

pub_date

1997-06-01 00:00:00

pages

519-22

issue

6

eissn

0036-5521

issn

1502-7708

journal_volume

32

pub_type

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