1,4-Benzodiazepine peripheral cholecystokinin (CCK-A) receptor agonists.
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.
Sherrill
R G
RG
Department of Medicinal Chemistry, Glaxo Welcome Research and Development, Research Triangle Park, NC 27709, USA. rgs13254@glaxowellcome.com
Berman
J M
JM
Birkemo
L
L
Croom
D K
DK
Dezube
M
M
Ervin
G N
GN
Grizzle
M K
MK
James
M K
MK
Johnson
M F
MF
Queen
K L
KL
Rimele
T J
TJ
Vanmiddlesworth
F
F
Sugg
E E
EE
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
D001067:Appetite Depressants; D043886:Receptor, Cholecystokinin A; D011949:Receptors, Cholecystokinin; D001569:Benzodiazepines