title: Synthesis and receptor binding affinity of cholecystokinin receptor ligands: 2-and 1-indolyl derivatives of PD134308.
abstract: 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.
authors.affiliation: Glaxo Wellcome S.p.A., Medicines Research Centre, Verona, Italy.
authors.forename: G
authors.initials: G
authors.lastname: Araldi
authors.forename: D
authors.initials: D
authors.lastname: Donati
authors.forename: B
authors.initials: B
authors.lastname: Oliosi
authors.forename: A
authors.initials: A
authors.lastname: Ursini
authors.forename: F
authors.initials: F
authors.lastname: van Amsterdam
authors.forename: B
authors.initials: B
authors.lastname: Natalini
authors.forename: R
authors.initials: R
authors.lastname: Pellicciari
authors.forename: G
authors.initials: G
authors.lastname: Tarzia
mesh_terms: 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
chemical_list: D006727:Hormone Antagonists; D007211:Indoles; D008024:Ligands; D011949:Receptors, Cholecystokinin; C065599:PD 134308; D008536:Meglumine