Abstract
Cholecystokinin (CCK) is a major gastrointestinal hormone with an important role in regulating various target organs such as pancreas, gallbladder and gut. CCK is also one of the most widely distributed neuropeptides in the brain and is considered as a putative central nervous system transmitter. The CCK receptors are divided into two CCK-A and CCK-B sub-type receptors. We have researched these respective receptor antagonists in the 1, 4-benzodiazepine derivatives and succeeded in discoveries of a selective CCK-A receptor antagonist, FK 480, a selective CCK-B receptor antagonist, FR 175985, and a dual CCK-A and -B receptor antagonist, FR 208419.This manuscript describes the syntheses and the structure-activity relationships of these respective CCK receptor antagonists.
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