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

by
de Tullio P, Delarge J, Pirotte B
Department of Medicinal Chemistry,
University of Liege, C.H.U.,
Tour 4-Niveau, 5, Avenue de 1'Hopital 1,
Liege, B-4000, Belgium.
Curr Med Chem 1999 Jun; 6(6):433-55


ABSTRACT

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.
SSRIs
Gepirone
Buspirone
Alprazolam
Adinazolam
Barbiturates
Benzodiazepines
Future anxiolytics
Drugs for treating GAD
Future pharmacotherapies
Cholecystokinin and anxiety


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