tetragastrin and asperlicin

The widespread involvement of the cholecystokinin-2/gastrin receptor (CCK

Topics: Animals; Benzodiazepinones; Clinical Trials as Topic; Furans; Humans; Lactams; Receptor, Cholecystokinin B; Structure-Activity Relationship; Sulfonamides; Tetragastrin

During the last few years, cholecystokinin (CCK) has emerged as an important hormone. This polypeptide has been located either in peripheral tissues such as the gastro-intestinal tract and the pancreas as well as in the central nervous system. High affinity CCK receptors are divided in two main subtypes: the CCK-A (A for (A for "alimentary") and the CCK-B (B for "brain") receptors. The latters are currently associated with the gastrin receptors. Since CCK is involved in many different biological processes such as gut function, digestive processes, control of feeding behaviour and neurotransmitter release, the therapeutical potential of cholecystokinin receptor ligands seems to be extremely broad and promising. Several families of CCK receptor ligands (peptides, peptidomimetics, peptoids or non-peptides) were prepared during 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 developments (since 1995) in the chemistry of CCK receptor ligands.

Topics: Animals; Anti-Anxiety Agents; Benzodiazepines; Benzodiazepinones; Humans; Indoles; Keto Acids; Ligands; Meglumine; Peptoids; Proglumide; Receptor, Cholecystokinin A; Receptor, Cholecystokinin B; Receptors, Cholecystokinin; Spiro Compounds; Structure-Activity Relationship; Tetragastrin