Cholecystokinin antagonists. Synthesis and biological evaluation of 4-substituted 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepines.
J Med Chem
; 31(1): 176-81, 1988 Jan.
Article
em En
| MEDLINE
| ID: mdl-3336017
ABSTRACT
A series of 4-substituted 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepines was prepared by standard methodology. These compounds were tested in vitro as antagonists of the binding of [125I]cholecystokinin (CCK) to rat pancreas and guinea pig brain receptors and of the binding of [125I]gastrin to guinea pig gastric glands. All compounds proved to have greater affinity for the peripheral CCK receptor with some analogues having IC50's in the subnanomolar range. In vivo activity of selected compounds in mice is presented and the structure/activity profile of this class of benzodiazepines as CCK antagonists is discussed.
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Base de dados:
MEDLINE
Assunto principal:
Triazóis
/
Benzodiazepinas
/
Colecistocinina
Limite:
Animals
Idioma:
En
Ano de publicação:
1988
Tipo de documento:
Article