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WIN 64821, a novel neurokinin antagonist produced by an Aspergillus sp. I. Fermentation and isolation

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journal contribution
posted on 1994-04-01, 00:00 authored by D M Sedlock, Colin BarrowColin Barrow, J E Brownell, A Hong, A M Gillum, D R Houck
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.

History

Journal

Journal of antibiotics

Volume

47

Issue

4

Pagination

391 - 398

Publisher

Japan Antibiotics Research Association

Location

Tokyo, Japan

ISSN

0021-8820

eISSN

1881-1469

Language

eng

Publication classification

C1.1 Refereed article in a scholarly journal

Copyright notice

1994, Japan Antibiotics Research Association