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Effects of guanyl nucleotides on CCKB receptor binding in brain tissue and continuous cell lines: a comparative study

R Kaufmann1, T Schöneberg, P Henklein

  • 1Friedrich-Schiller-University Jena, Germany.

Neuropeptides
|July 1, 1995
PubMed

Insights

Non-hydrolyzable guanyl nucleotide analogue, GTP-gamma S, inhibits CCK-B receptor binding across various cell types. This suggests CCK-B receptors are coupled to G-proteins similarly in human and animal tissues.

Area of Science:

  • Pharmacology
  • Neuroscience
  • Cell Biology

Background:

  • The cholecystokinin B receptor (CCK-BR) plays a role in various physiological processes.
  • Understanding CCK-BR signaling is crucial for developing targeted therapies.
  • G-protein coupling is a key mechanism for receptor signal transduction.

Purpose of the Study:

  • To investigate the effect of GTP-gamma S on CCK-BR binding.
  • To determine if CCK-BR exhibits G-protein coupling across different cell models.

Main Methods:

  • Utilized [3H]CCK-8S saturation and competition binding assays.
  • Tested the effects of GTP-gamma S on CCK-BR binding in human/guinea-pig cortex, Jurkat T-cells, GH3 cells, C6 cells, and NCI-H69 cells.

Main Results:

  • GTP-gamma S inhibited specific [3H]CCK-8S binding in a concentration-dependent manner.
  • A plateau in inhibition was observed at 10-25 microM GTP-gamma S.
  • GTP-gamma S increased Kd and IC50 values, while Bmax remained unaffected across all tested CCK-BR models.

Conclusions:

  • CCK-B receptors are consistently G-protein coupled in diverse cellular systems.
  • These findings support a conserved G-protein coupling mechanism for CCK-BR.

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