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噻吩衍生物：一类新型强效去甲肾上腺素和5-羟色胺再摄取抑制剂

Thiophene derivatives: a new series of potent norepinephrine and serotonin reuptake inhibitors.

作者信息

Zhang Ao, Zhou Guochun, Rong Suo-Bao, Johnson Kenneth M, Zhang Mei, Kozikowski Alan P

机构信息

Drug Discovery Program, Department of Neurology, Georgetown University Medical Center, 3900 Reservoir Road, NW, Washington, DC 20007-2197, USA.

出版信息

Bioorg Med Chem Lett. 2002 Apr 8;12(7):993-5. doi: 10.1016/s0960-894x(02)00103-8.

DOI:10.1016/s0960-894x(02)00103-8
PMID:11909701
Abstract

A series of (1S,3S,6R,10S)-(Z)-9-(thienylmethylene- or substituted thienylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes was prepared and evaluated for the ability to block dopamine, serotonin, and norepinephrine reuptake by their respective transporters. Compound 5b is a NET-selective inhibitor, 5c is a mixed NET- and SERT-selective inhibitor, while 11 is a SERT-selective inhibitor.

摘要

制备了一系列(1S,3S,6R,10S)-(Z)-9-(噻吩基亚甲基或取代噻吩基亚甲基)-7-氮杂三环[4.3.1.0(3,7)]癸烷，并评估了它们通过各自转运体阻断多巴胺、5-羟色胺和去甲肾上腺素再摄取的能力。化合物5b是一种去甲肾上腺素转运体（NET）选择性抑制剂，5c是一种NET和5-羟色胺转运体（SERT）混合选择性抑制剂，而11是一种SERT选择性抑制剂。

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