title: 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.
  
  
  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.
authors.affiliation: Laboratory of Endocrinology, Gastroenterology, and Oncology, Faculty of Medicine, Norwegian University of Science and Technology, Trondheim, Norway.
authors.forename: R
authors.initials: R
authors.lastname: Marvik
authors.forename: A K
authors.initials: AK
authors.lastname: Sandvik
authors.forename: H L
authors.initials: HL
authors.lastname: Waldum
mesh_terms: 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*
chemical_list: D005755:Gastrins; D006727:Hormone Antagonists; D007211:Indoles; D034444:Peptoids; D043887:Receptor, Cholecystokinin B; D011949:Receptors, Cholecystokinin; C065599:PD 134308; D008536:Meglumine