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WIN 64821，一种由曲霉属真菌产生的新型神经激肽拮抗剂。I. 发酵与分离。

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

作者信息

Sedlock D M, Barrow C J, Brownell J E, Hong A, Gillum A M, Houck D R

机构信息

Sterling Winthrop Pharmaceuticals Research Division, Collegeville, PA 19426-0900.

出版信息

J Antibiot (Tokyo). 1994 Apr;47(4):391-8. doi: 10.7164/antibiotics.47.391.

DOI:10.7164/antibiotics.47.391
PMID:7515037
Abstract

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.

摘要

WIN 64821是一种非肽类神经激肽拮抗剂，从一株曲霉属真菌SC319中分离得到。该化合物在不同的发酵培养基中产生，当培养物在添加了L-色氨酸和L-苯丙氨酸的合成培养基中生长时，产量最高。发酵6天后，产量超过600毫克/升。在培养提取物中还鉴定出了WIN 64821的两种类似物，并随后对其生物活性进行了测试。WIN 64821是从该培养物中分离得到的最有效的化合物，作为一种P物质结合抑制剂，对人神经激肽1受体具有亚微摩尔效力。

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