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首页> 外文期刊>The Journal of Antibiotics: An International Journal >(2R-trans)-2-Butyl-5-heptylpyrrolidine as a Potent Sigma Receptor Ligand Produced by Streptomyces longispororuber
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(2R-trans)-2-Butyl-5-heptylpyrrolidine as a Potent Sigma Receptor Ligand Produced by Streptomyces longispororuber

机译:(2R-反式)-2-丁基-5-庚基吡咯烷作为长链霉菌产生的有效Sigma受体配体

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摘要

A potent sigma (#sigma#)receptor ligand was isolated from the cultrue 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 IC_(50) 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.
机译:从长链霉菌(Streptomyces longispororuber)#525的培养液中分离了有效的sigma(#sigma#)受体配体。活性化合物经光谱和化学研究鉴定为(2R-反式)-2-丁基-5-庚基吡咯烷。该化合物对#sigma#受体表现出高亲和力和选择性。朝向#sigma#_1,#sigma#_2和多巴胺D_2受体的IC_(50)值分别为2.0、22.7和大于40,000 nM。还发现合成的(2S-反式)-和(+-)-顺式异构体是高亲和力的#sigma#配体。

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