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.
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.
Satoh
M
M
Neuroscience/Gastrointestinal Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd., Ibaraki, Japan.
Okamoto
Y
Y
Koshio
H
H
Ohta
M
M
Nishida
A
A
Akuzawa
S
S
Miyata
K
K
Mase
T
T
Semple
G
G
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
D006727:Hormone Antagonists; D011949:Receptors, Cholecystokinin; D001569:Benzodiazepines; C087260:YM 022; D002766:Cholecystokinin