Cholecystokinin (CCK) and gastrin are gastrointestinal polypeptide hor
mones that exert several regulatory functions on motility and secretio
n in the gastrointestinal tract. Their biological functions are mediat
ed by different receptors located on the target tissues. Several selec
tive and potent nonpeptide CCKB/gastrin receptor antagonists have been
synthesized and are currently being studied. This review describes th
e development of different classes oi these antagonists, and looks at
future potential therapeutic benefits of such agents.