A Potent Nonpeptide Cholecystokinin Antagonist Selective for Peripheral Tissues Isolated from Aspergillus alliaceus

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 i...

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Bibliographic Details
Published in:Science (American Association for the Advancement of Science) 1985-10, Vol.230 (4722), p.177-179
Main Authors: Raymond S. L. Chang, Lotti, Victor J., Monaghan, Richard L., Birnbaum, Jerome, Stapley, Edward O., Goetz, Michael A., Albers-Schönberg, Georg, Patchett, Arthur A., Liesch, Jerrold M., Hensens, Otto D., Springer, James P.
Format: Article
Language:English
Subjects:
Agonists
Animals
Aspergillus
Aspergillus - metabolism
Benzodiazepinones - isolation & purification
Benzodiazepinones - pharmacology
Biological and medical sciences
Brain
Chemical Phenomena
Chemistry
Cholecystokinin
Cholecystokinin - antagonists & inhibitors
Cholecystokinin - pharmacology
Cholecystokinin - physiology
Cholecystokinin receptors
Dose-Response Relationship, Drug
Drugs
Gallbladder
Gallbladder - drug effects
General pharmacology
Guinea Pigs
Guinea pigs as laboratory animals
Ileum
Ileum - drug effects
Inhibitory concentration 50
Laboratory animals
Medical sciences
Neuropeptides
Pancreas - drug effects
Pharmacology. Drug treatments
Physicochemical properties. Structure-activity relationships
Physiological aspects
Rats
Receptors
Receptors, Cell Surface - drug effects
Receptors, Cholecystokinin
Research and development laboratories
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Summary: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.
ISSN:0036-8075
1095-9203
DOI:10.1126/science.2994227