title: 1,4-Benzodiazepine peripheral cholecystokinin (CCK-A) receptor agonists.
abstract: A series of 1,4-benzodiazepines, N-1-substituted with an N-isopropyl-N-phenylacetamide moiety, was synthesized and screened for CCK-A agonist activity. In vitro agonist activity on isolated guinea pig gallbladder along with in vivo induction of satiety following intraperitoneal administration in a rat feeding assay was demonstrated.
authors.affiliation: Department of Medicinal Chemistry, Glaxo Welcome Research and Development, Research Triangle Park, NC 27709, USA. rgs13254@glaxowellcome.com
authors.forename: R G
authors.initials: RG
authors.lastname: Sherrill
authors.forename: J M
authors.initials: JM
authors.lastname: Berman
authors.forename: L
authors.initials: L
authors.lastname: Birkemo
authors.forename: D K
authors.initials: DK
authors.lastname: Croom
authors.forename: M
authors.initials: M
authors.lastname: Dezube
authors.forename: G N
authors.initials: GN
authors.lastname: Ervin
authors.forename: M K
authors.initials: MK
authors.lastname: Grizzle
authors.forename: M K
authors.initials: MK
authors.lastname: James
authors.forename: M F
authors.initials: MF
authors.lastname: Johnson
authors.forename: K L
authors.initials: KL
authors.lastname: Queen
authors.forename: T J
authors.initials: TJ
authors.lastname: Rimele
authors.forename: F
authors.initials: F
authors.lastname: Vanmiddlesworth
authors.forename: E E
authors.initials: EE
authors.lastname: Sugg
mesh_terms: D000818:Animals; D001067:Appetite Depressants / Q000138:chemical synthesis* / Q000494:pharmacology*; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000494:pharmacology*; D005704:Gallbladder / Q000187:drug effects; D006168:Guinea Pigs; D066298:In Vitro Techniques; D051381:Rats; D020318:Rats, Long-Evans; D043886:Receptor, Cholecystokinin A; D011949:Receptors, Cholecystokinin / Q000819:agonists*; D012528:Satiety Response / Q000187:drug effects
chemical_list: D001067:Appetite Depressants; D043886:Receptor, Cholecystokinin A; D011949:Receptors, Cholecystokinin; D001569:Benzodiazepines