(2R-trans)-2-butyl-5-heptylpyrrolidine as a potent sigma receptor ligand produced by Streptomyces longispororuber

被引：12

作者：

Kumagai, K

Shono, K

Nakayama, H

Ohno, Y

Saji, I

机构：

[1] Sumitomo Pharmaceut Co Ltd, Res Ctr, Exploratory Res Grp, Takarazuka, Hyogo 6650051, Japan

[2] Sumitomo Pharmaceut Co Ltd, Res Ctr, Discovery Res Labs 1, Konohana Ku, Osaka 5540022, Japan

来源：

JOURNAL OF ANTIBIOTICS | 2000年 / 53卷 / 05期

关键词：

D O I：

10.7164/antibiotics.53.467

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

A potent sigma (sigma) receptor ligand was isolated from the culture broth of Streptomyces longispororuber #525. The active compound was identified to be (2R-trans)-2-butyl-5-heptylpyrrolidine by spectroscopic and chemical studies. The compound exhibited high affinity and selectivity for sigma receptors. The IC50 values toward sigma(1), sigma(2) and dopamine D-2 receptors were 2.0, 22.7 and more than 40,000 nM, respectively. Its (2S-trans)- and (+/-)-cis-isomers, both synthesized, were also found to be high affinity sigma ligands.

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页码：467 / 473

页数：7

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