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


CONCLUSIONS
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.
Marvik
R
R
Laboratory of Endocrinology, Gastroenterology, and Oncology, Faculty of Medicine, Norwegian University of Science and Technology, Trondheim, Norway.
Sandvik
A K
AK
Waldum
H L
HL
D000818:Animals; D005744:Gastric Acid / Q000378:metabolism; D005755:Gastrins / Q000819:agonists*; D006636:Histamine Release / Q000187:drug effects; D006727:Hormone Antagonists / Q000494:pharmacology*; D007211:Indoles / Q000494:pharmacology*; D008297:Male; D008536:Meglumine / Q000031:analogs & derivatives* / Q000494:pharmacology; D034444:Peptoids; D010477:Perfusion; D051381:Rats; D017208:Rats, Wistar; D043887:Receptor, Cholecystokinin B; D011949:Receptors, Cholecystokinin / Q000187:drug effects; D013270:Stomach / Q000187:drug effects*
D005755:Gastrins; D006727:Hormone Antagonists; D007211:Indoles; D034444:Peptoids; D043887:Receptor, Cholecystokinin B; D011949:Receptors, Cholecystokinin; C065599:PD 134308; D008536:Meglumine