title: Biological activity of analogues of YM022. Novel (3-amino substituted phenyl)urea derivatives of 1,4-benzodiazepin-2-one as gastrin/cholecystokinin-B receptor antagonists.
abstract: A series of (3-substituted phenyl)urea analogues of the potent gastrin/cholecystokinin (CCK)-B receptor antagonist YM022 has been prepared. Structure-activity relationship studies of this series suggested that a number of analogues retained good in vitro potency for gastrin/CCK-B receptor. In particular, the (3-amino substituted phenyl)urea derivatives (10-12) were more potent inhibitors of pentagastrin-induced gastric acid secretion in rats than YM022 on intraduodenal (i.d.) administration.
authors.affiliation: Neuroscience/Gastrointestinal Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd., Ibaraki, Japan.
authors.forename: M
authors.initials: M
authors.lastname: Satoh
authors.forename: Y
authors.initials: Y
authors.lastname: Okamoto
authors.forename: H
authors.initials: H
authors.lastname: Koshio
authors.forename: M
authors.initials: M
authors.lastname: Ohta
authors.forename: A
authors.initials: A
authors.lastname: Nishida
authors.forename: S
authors.initials: S
authors.lastname: Akuzawa
authors.forename: K
authors.initials: K
authors.lastname: Miyata
authors.forename: T
authors.initials: T
authors.lastname: Mase
authors.forename: G
authors.initials: G
authors.lastname: Semple
mesh_terms: D000818:Animals; D001569:Benzodiazepines / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D001921:Brain / Q000378:metabolism; D002766:Cholecystokinin / Q000378:metabolism; D005744:Gastric Acid / Q000378:metabolism; D005753:Gastric Mucosa / Q000378:metabolism; D006727:Hormone Antagonists / Q000378:metabolism / Q000494:pharmacology*; D010179:Pancreas / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D011949:Receptors, Cholecystokinin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013270:Stomach / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D006727:Hormone Antagonists; D011949:Receptors, Cholecystokinin; D001569:Benzodiazepines; C087260:YM 022; D002766:Cholecystokinin