sincalide and oltipraz

The synthesis of lipophylic derivatives of the amino acid residues of the CCK-8 fragment is described. According to "in vitro" binding studies and functional test, nearly all the compounds behaves as CCK-antagonists; moreover some compounds are able to interact differentially with CCK-A and CCK-B receptor subtype. In particular, compounds 2c, 2g, and 2h possess a high affinity for the CCK-A receptor subtype coupled with a low affinity for the CCK-B subtype. This results in an interesting selectivity profile. However, the same compounds are not able to antagonize the effects exerted by CCK-itself, when tested in "in vivo" assays.

Topics: Amino Acid Sequence; Animals; Brain Chemistry; Cholecystokinin; Female; Gallbladder; Guinea Pigs; In Vitro Techniques; Male; Mice; Molecular Sequence Data; Pancreas; Pyrazines; Receptors, Cholecystokinin; Sincalide; Thiones; Thiophenes; Vinyl Compounds