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 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.
D000818:Animals; D001230:Aspergillus / Q000378:metabolism*; D001570:Benzodiazepinones / Q000302:isolation & purification* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D002766:Cholecystokinin / Q000037:antagonists & inhibitors* / Q000494:pharmacology / Q000502:physiology; D004305:Dose-Response Relationship, Drug; D005704:Gallbladder / Q000187:drug effects; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D010179:Pancreas / Q000187:drug effects; D051381:Rats; D011956:Receptors, Cell Surface / Q000187:drug effects; D011949:Receptors, Cholecystokinin
D001570:Benzodiazepinones; D011956:Receptors, Cell Surface; D011949:Receptors, Cholecystokinin; D002766:Cholecystokinin; C046367:asperlicin