Characterization of neuronal cholecystokinin receptor by L-364,718 in Auerbach's plexus

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Abstract

The release of [3H]acetylcholine ([3H]ACh) from Auerbach's plexus and the contraction of longitudinal muscle strips in response to the administration of cholecystokinin (CCK) were measured and recorded simultaneously. The peripheral CCK receptor antagonist, 3S(-)-N-(2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepine-3-yl)-1Hindole-2-carboxamide (L-364,718), antagonized the ACh releasing effect of CCK in a dose-dependent manner. The IC50 value and the dissociation constant (KD) were 41.0 ± 2.0 pM and 0.06 ± 0.01 nM, respectively. These results suggest that L-364,718 is a very potent antagonist of the neuronal CCK receptors.

Original languageEnglish
Pages (from-to)101-104
Number of pages4
JournalEuropean Journal of Pharmacology
Volume178
Issue number1
DOIs
Publication statusPublished - Mar 13 1990

Keywords

  • Acetylcholine release
  • Cholecystokinin
  • L-364,718
  • Myenteric plexus
  • Neuronal cholecystokinin receptors

ASJC Scopus subject areas

  • Pharmacology

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