A potent nonpeptide cholecystokinin antagonist selective for peripheral tissues isolated from Aspergillus alliaceus.

نویسندگان

  • R S Chang
  • V J Lotti
  • R L Monaghan
  • J Birnbaum
  • E O Stapley
  • M A Goetz
  • G Albers-Schönberg
  • A A Patchett
  • J M Liesch
  • O D Hensens
چکیده

A new, competitive, nonpeptide cholecystokinin (CCK) antagonist, asperlicin, was isolated from the fungus Aspergillus alliaceus. The compound has 300 to 400 times the affinity for pancreatic, ileal, and gallbladder CCK receptors than proglumide, a standard agent of this class. Moreover, asperlicin is highly selective for peripheral CCK receptors relative to brain CCK and gastrin receptors. Since asperlicin also exhibits long-lasting CCK antagonist activity in vivo, it should provide a valuable tool for investigating the physiological and pharmacological actions of CCK.

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Asperlicin, a novel non-peptidal cholecystokinin antagonist from Aspergillus alliaceus. Fermentation, isolation and biological properties.

The fermentation and isolation of a new, non-peptide cholecystokinin antagonist, asperlicin, produced by Aspergillus alliaceus is described. The potent and specific interaction of asperlicin with cholecystokinin receptors was shown using in vitro biochemical assays.

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عنوان ژورنال:
  • Science

دوره 230 4722  شماره 

صفحات  -

تاریخ انتشار 1985