Synthesis and receptor binding affinity of cholecystokinin receptor ligands: 2-and 1-indolyl derivatives of PD134308.
The synthesis of two "dipeptoids" structurally related to the CCK-B antagonist CI-988 (PD134308) is described. The 2- and 1-indolyl derivatives 4a, b were prepared in order to define the role of the tryptophan moiety in this series of "dipeptoids". They were evaluated as competitors in the binding of [3H]-CCK8S on guinea pig brain CCK-B receptors.
Araldi
G
G
Glaxo Wellcome S.p.A., Medicines Research Centre, Verona, Italy.
Donati
D
D
Oliosi
B
B
Ursini
A
A
van Amsterdam
F
F
Natalini
B
B
Pellicciari
R
R
Tarzia
G
G
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001923:Brain Chemistry / Q000187:drug effects; D006168:Guinea Pigs; D006727:Hormone Antagonists / Q000138:chemical synthesis / Q000494:pharmacology*; D006868:Hydrolysis; D066298:In Vitro Techniques; D007211:Indoles / Q000138:chemical synthesis / Q000494:pharmacology*; D008024:Ligands; D008297:Male; D008536:Meglumine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D011949:Receptors, Cholecystokinin / Q000037:antagonists & inhibitors*; D013055:Spectrophotometry, Infrared
D006727:Hormone Antagonists; D007211:Indoles; D008024:Ligands; D011949:Receptors, Cholecystokinin; C065599:PD 134308; D008536:Meglumine