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Abstract
The discovery of the benzodiazepine cholecystokinin (CCK) antagonists played a major role in clarifying the pharmacology of the 33-amino acid peptide hormone CCK. The recent appreciation of the potential role of CCK-B receptors in panic disorder, anxiety, pain, and psychosis has led to a reappraisal of the initial benzodiazepine SAR studies to afford new antagonists with improved pharmacokinetic properties. The resulting plethora of new CCK-B receptor antagonists will serve to evaluate the role of CCK-B receptor activation in human disease through clinical study.