Recent advances in the chemistry of cholecystokinin receptor ligands (agonists and antagonists)

During the last few years, cholecystokinin (CCK) has emerged as an importan t hormone. This polypeptide has been located either in peripheral tissues s uch as the gastro intestinal tract and the pancreas as well as in the centr al nervous system. High affinity CCK receptors are divided in two main subt ypes: the CCK-A (A for "alimentary") and the CCK-B (B for "brain") receptor s. The tatters are currently associated with the gastrin receptors. Since C CK is involved in many different biological processes such as gut function, digestive processes, control of feeding behaviour and neurotransmitter rel ease, the therapeutical potential of cholecystokinin receptor ligands seems to be extremely broad and promising. Several families of CCK receptor liga nds (peptides, peptidomimetics, peptoids or non-peptides) were prepared dur ing the last twenty years. The main goal of these researches was to improve agonistic or antagonistic potency but also to find selective compounds for a specific CCK receptor subtype. This review presents the recent developme nts (since 1995) in the chemistry of CCK receptor ligands.