Document Detail


WIN 64821, a novel neurokinin antagonist produced by an Aspergillus sp. I. Fermentation and isolation.
MedLine Citation:
PMID:  7515037     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
WIN 64821, a nonpeptide neurokinin antagonist, was isolated from a strain of Aspergillus sp., SC319. The compound was produced in different fermentation media with greatest yields observed when the culture was grown in a synthetic medium supplemented with L-tryptophan and L-phenylalanine. After 6 days fermentation, yields greater than 600 mg/liter were obtained. Two analogs of WIN 64821 were also identified in the culture extracts and subsequently tested for biological activity. WIN 64821 was the most potent compound isolated from this culture and exhibited activity as a substance P-binding inhibitor with submicromolar potency against the human neurokinin 1 receptor.
Authors:
D M Sedlock; C J Barrow; J E Brownell; A Hong; A M Gillum; D R Houck
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  The Journal of antibiotics     Volume:  47     ISSN:  0021-8820     ISO Abbreviation:  J. Antibiot.     Publication Date:  1994 Apr 
Date Detail:
Created Date:  1994-06-30     Completed Date:  1994-06-30     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  0151115     Medline TA:  J Antibiot (Tokyo)     Country:  JAPAN    
Other Details:
Languages:  eng     Pagination:  391-8     Citation Subset:  IM    
Affiliation:
Sterling Winthrop Pharmaceuticals Research Division, Collegeville, PA 19426-0900.
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MeSH Terms
Descriptor/Qualifier:
Aspergillus / classification,  growth & development,  metabolism*
Astrocytoma / metabolism
Binding Sites
Chromatography, High Pressure Liquid
Culture Media
Fermentation
Humans
Indoles / chemistry,  isolation & purification*,  metabolism,  pharmacology
Piperazines / chemistry,  isolation & purification*,  metabolism,  pharmacology
Spectrometry, Mass, Fast Atom Bombardment
Substance P / antagonists & inhibitors*,  metabolism
Tryptophan / chemistry
Tumor Cells, Cultured
Chemical
Reg. No./Substance:
0/Culture Media; 0/Indoles; 0/Piperazines; 150881-27-9/WIN 64821; 33507-63-0/Substance P; 73-22-3/Tryptophan

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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