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Bellier, B ; Million, ME ; DaNascimento, S ; Meudal, H ; Kellou, S ; Maigret, B ; Garbay, C

Replacement of glycine with dicarbonyl and related moieties in analogues of the C-terminal pentapeptide of cholecystokinin : CCK2 agonists displaying a novel binding mode

Journal of Medicinal Chemistry 43 (20) 3614-3623

par Administrateur - publié le

Abstract :

Recent advances in the field of cholecystokinin have indicated the possible occurrence of multiple affinity states of the CCK2 receptor. Besides, numerous pharmacological experiments performed "in vitro" and "in vivo" support the eventuality of different pharmacological profiles associated to CCK2 ligands. Indeed, some agonists are essentially anxiogenic and uneffective in memory tests, whereas others are not anxiogenic and appear as able to reinforce memory. The reference compound for the latter profile is the CCK-8 analogue BC 264 (Boc-Tyr(SO3H)-gnle-mGly-Trp-(NMe)Nle-Asp-Phe-NH2).