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Related Experiment Videos

CCK receptor antagonists

J Dunlop1

  • 1CNS Disorders, Wyeth-Ayerst Research, Princeton, NJ 08543, USA. Dunlopj@war.wyeth.com

General Pharmacology
|October 29, 1998
PubMed
Summary
This summary is machine-generated.

Cholecystokinin (CCK) receptors, CCK-A and CCK-B, are key drug targets. Benzodiazepine-based compounds like L-365,260, L-740,093, and YM022 show selective CCK-B receptor antagonism, offering potential therapeutic applications.

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Gastroenterology

Background:

  • Cholecystokinin (CCK) is a peptide hormone and neurotransmitter found in the gut and brain, regulating various biological functions.
  • Two CCK receptor subtypes, CCK-A and CCK-B, have been identified, with CCK-A predominant peripherally and CCK-B centrally, though both have discrete distributions.
  • CCK receptors are significant targets for therapeutic intervention in various physiological processes.

Purpose of the Study:

  • To characterize subtype-selective CCK receptor antagonists.
  • To investigate the in vitro pharmacological profiles of novel benzodiazepine-based CCK-B receptor antagonists.
  • To evaluate the competitive and insurmountable antagonism properties of L-365,260, L-740,093, and YM022.

Main Methods:

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  • Pharmacological characterization and molecular cloning of CCK receptor subtypes.
  • In vitro assays using human CCK-B receptor expressed in CHO cells.
  • Assessment of competitive and insurmountable antagonism of CCK-B receptor antagonists.

    • Main Results:

    • The benzodiazepine derivatives L-365,260, L-740,093, and YM022 were identified as selective CCK-B receptor antagonists.
    • L-365,260 demonstrated competitive antagonism at the CCK-B receptor.
    • L-740,093 and YM022 exhibited insurmountable antagonism at the CCK-B receptor in vitro.

    Conclusions:

    • Benzodiazepine derivatives represent a promising class of selective CCK-B receptor antagonists.
    • These compounds, particularly L-740,093 and YM022, display distinct antagonism profiles.
    • Further research into these antagonists may yield novel therapeutic agents targeting CCK-mediated pathways.