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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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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container_end_page 179
container_issue 4722
container_start_page 177
container_title Science (American Association for the Advancement of Science)
container_volume 230
creator 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.
description 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.
doi_str_mv 10.1126/science.2994227
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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.</creator><creatorcontrib>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.</creatorcontrib><description>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. 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L. Chang</creatorcontrib><creatorcontrib>Lotti, Victor J.</creatorcontrib><creatorcontrib>Monaghan, Richard L.</creatorcontrib><creatorcontrib>Birnbaum, Jerome</creatorcontrib><creatorcontrib>Stapley, Edward O.</creatorcontrib><creatorcontrib>Goetz, Michael A.</creatorcontrib><creatorcontrib>Albers-Schönberg, Georg</creatorcontrib><creatorcontrib>Patchett, Arthur A.</creatorcontrib><creatorcontrib>Liesch, Jerrold M.</creatorcontrib><creatorcontrib>Hensens, Otto D.</creatorcontrib><creatorcontrib>Springer, James P.</creatorcontrib><title>A Potent Nonpeptide Cholecystokinin Antagonist Selective for Peripheral Tissues Isolated from Aspergillus alliaceus</title><title>Science (American Association for the Advancement of Science)</title><addtitle>Science</addtitle><description>A new, competitive, nonpeptide cholecystokinin (CCK) antagonist, asperlicin, was isolated from the fungus Aspergillus alliaceus. 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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.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c675t-9354822ef7b458792144f2cf02fbc3092ef61af4c4b807c87f6ac728d2ca6c073</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1985</creationdate><topic>Agonists</topic><topic>Animals</topic><topic>Aspergillus</topic><topic>Aspergillus - metabolism</topic><topic>Benzodiazepinones - isolation &amp; purification</topic><topic>Benzodiazepinones - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Brain</topic><topic>Chemical Phenomena</topic><topic>Chemistry</topic><topic>Cholecystokinin</topic><topic>Cholecystokinin - antagonists &amp; inhibitors</topic><topic>Cholecystokinin - pharmacology</topic><topic>Cholecystokinin - physiology</topic><topic>Cholecystokinin receptors</topic><topic>Dose-Response Relationship, Drug</topic><topic>Drugs</topic><topic>Gallbladder</topic><topic>Gallbladder - drug effects</topic><topic>General pharmacology</topic><topic>Guinea Pigs</topic><topic>Guinea pigs as laboratory animals</topic><topic>Ileum</topic><topic>Ileum - drug effects</topic><topic>Inhibitory concentration 50</topic><topic>Laboratory animals</topic><topic>Medical sciences</topic><topic>Neuropeptides</topic><topic>Pancreas - drug effects</topic><topic>Pharmacology. 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L. Chang</au><au>Lotti, Victor J.</au><au>Monaghan, Richard L.</au><au>Birnbaum, Jerome</au><au>Stapley, Edward O.</au><au>Goetz, Michael A.</au><au>Albers-Schönberg, Georg</au><au>Patchett, Arthur A.</au><au>Liesch, Jerrold M.</au><au>Hensens, Otto D.</au><au>Springer, James P.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>A Potent Nonpeptide Cholecystokinin Antagonist Selective for Peripheral Tissues Isolated from Aspergillus alliaceus</atitle><jtitle>Science (American Association for the Advancement of Science)</jtitle><addtitle>Science</addtitle><date>1985-10-11</date><risdate>1985</risdate><volume>230</volume><issue>4722</issue><spage>177</spage><epage>179</epage><pages>177-179</pages><issn>0036-8075</issn><eissn>1095-9203</eissn><coden>SCIEAS</coden><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.</abstract><cop>Washington, DC</cop><pub>The American Association for the Advancement of Science</pub><pmid>2994227</pmid><doi>10.1126/science.2994227</doi><tpages>3</tpages></addata></record>
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identifier ISSN: 0036-8075
ispartof Science (American Association for the Advancement of Science), 1985-10, Vol.230 (4722), p.177-179
issn 0036-8075
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source JSTOR Archival Journals and Primary Sources Collection【Remote access available】; Science Online科学在线
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
title A Potent Nonpeptide Cholecystokinin Antagonist Selective for Peripheral Tissues Isolated from Aspergillus alliaceus
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