A potent nonpeptide cholecystokinin antagonist selective for peripheral tissues isolated from Aspergillus alliaceus
Authors:
- R. ChangRCR. Chang
- V. LottiVLV. Lotti
- R. MonaghanRMR. Monaghan
- J BirnbaumJBJ Birnbaum
- E. StapleyESE. Stapley
- M. GoetzMGM. Goetz
- G Albers-SchonbergGAG Albers-Schonberg
- A. PatchettAPA. Patchett
- J. LieschJLJ. Liesch
- O. HensensOHO. Hensens
- Al. EtAEAl. Et
- 11 October 1985
- journal article
- research article
- Published by American Association for the Advancement of Science (AAAS) in Science
- Vol. 230 (4722) , 177-179
Abstract
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.Keywords
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