title: Synthesis of cyclic analogues of cholecystokinin highly selective for central receptors.
abstract: Cyclic CCK analogues in which positions 28 and 31 have been replaced by lysine residues and whose side chains are bridged by a succinic moiety, were synthesized. They were tested for their ability to inhibit the binding of 125I-BH-CCK-8 to isolated rat pancreatic acini and to guinea pig brain membranes. These cyclic CCK-analogues were compared to the potent CCK analogue Boc-[Nle28,31]-CCK-7 and to Boc-Trp-Leu-Asp-Phe-NH2, analogue of CCK-4. These cyclic compounds appeared to be highly selective for central CCK receptors.
authors.affiliation: CNRS-INSERM Center for Pharmacology and Endocrinology, Montpellier, France.
authors.forename: M
authors.initials: M
authors.lastname: Rodriguez
authors.forename: M
authors.initials: M
authors.lastname: Amblard
authors.forename: M C
authors.initials: MC
authors.lastname: Galas
authors.forename: M F
authors.initials: MF
authors.lastname: Lignon
authors.forename: A
authors.initials: A
authors.lastname: Aumelas
authors.forename: J
authors.initials: J
authors.lastname: Martinez
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism; D055598:Chemical Phenomena; D002621:Chemistry; D002766:Cholecystokinin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism; D003500:Cyclization; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D008969:Molecular Sequence Data; D015394:Molecular Structure; D010179:Pancreas / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D011949:Receptors, Cholecystokinin / Q000378:metabolism*
chemical_list: D011949:Receptors, Cholecystokinin; D002766:Cholecystokinin