Cholecystokinin Receptor Antagonists In Vitro

  • R. T. Jensen
  • J. D. Gardner


Since the original observation in 1979 [48] that dibutyryl cyclic GMP (Bt2cGMP) functions as a weak, but specific, cholecystokinin (CCK) receptor antagonist, five different classes of CCK receptor antagonists have been described in various in vitro studies (Tables 1, 2) [30,31]. Members of at least two of these classes [i.e., amino acid derivatives such as lorglumide (CR 1409) or loxiglumide (CR 1505) and substituted benzodiazepine analogues such as L-364718 (MK-329), L-365260 or A-65186 have sufficient potency and specificity to be generally useful for in vivo studies that explore the importance of CCK-related peptides in various physiological processes. It is likely that additional useful CCK receptor antagonists which may further distinguish CCK receptor subtypes or have higher potency, will be developed, probably from one of the five different classes currently described. In this chapter the results of in vitro studies with each of the different classes of CCK receptor antagonists are reviewed.


Pancreatic Acinar Cell Pancreatic Acinus Amylase Release Cholecystokinin Receptor Gastrin Receptor 
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Copyright information

© Springer-Verlag Berlin Heidelberg 1991

Authors and Affiliations

  • R. T. Jensen
  • J. D. Gardner
    • 1
  1. 1.Digestive Diseases Branch, National Institutes of Diabetes and Digestive and Kidney DiseasesNational Institutes of HealthBethesdaUSA

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