Cholecystokinin-A receptor antagonists: therapies for gastrointestinal disorders

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Abstract
Cholecystokinin (CCK) is a peptide that exerts several regulatory functions in the periphery, as well as in the brain. The biological functions attributed to CCK are mediated by two receptor subtypes, termed CCKA and CCKB, located predominantly in the gastrointestinal (GI) tract and in the brain, respectively. Several selective and potent non-petide CCKA receptor antagonists have been synthesised and fully characterised in preclinical studies. A few of them have been, and continue to be tested in humans. This paper focuses on the data available on the effect of CCKA receptor antagonist administration in humans, and shows how, in addition to allowing a more exact definition of the role of CCK in the regulation of some GI functions, these drugs may also possess therapeutic potential in GI disorders.