Localization of peripheral cholecystokinin receptors in vivo using the cholecystokinin antagonist [3H](±)-MK-329

B. Sadzot, J. Sheldon, R. F. Dannals, H. T. Ravert, H. N. Wagner, J. J. Frost

Research output: Contribution to journalArticle

Abstract

Cholecystokinin (CCK) regulates various gastrointestinal functions through specific receptors. The mechanisms responsible for disorders of these functions could be elucidated by non-invasively localizing CCK receptors and quantifying their number in vivo. MK-329 is a highly selective and very high affinity antagonist at the peripheral CCK receptor. We investigated the in vivo binding of [3H](±)-MK-329 in mice to determine if binding to CCK receptors could be detected after systemic administration of the tracer. The uptake of [3H](±)-MK-329 increased in the pancreas from 5 min to 4 h after administration. The binding was saturable, stereospecific, and more than 80% specific. A total/non-specific binding ratio of 43 was reached at 8 h post-injection. The pancreas was the only organ where specific binding could be detected. Our results suggest that MK-329 labeled with a positron emitter such as C-11 could be used with positron emission tomography to image and quantify peripheral CCK receptors in man.

Original languageEnglish (US)
Pages (from-to)195-201
Number of pages7
JournalEuropean Journal of Pharmacology
Volume185
Issue number2-3
DOIs
StatePublished - Aug 28 1990

Keywords

  • (In vivo binding)
  • CCK receptor antagonists
  • CCK receptors (peripheral)
  • MK-329
  • PET (positron emission tomography)
  • Pancreas

ASJC Scopus subject areas

  • Pharmacology

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