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二价生物胺再摄取抑制剂

Bivalent biogenic amine reuptake inhibitors.

作者信息

Fandrick Keith, Feng Xianqi, Janowsky Aaron, Johnson Robert, Cashman John R

机构信息

Human BioMolecular Research Institute, 5310 Eastgate Mall, 92121, San Diego, CA, USA.

出版信息

Bioorg Med Chem Lett. 2003 Jul 7;13(13):2151-4. doi: 10.1016/s0960-894x(03)00386-x.

DOI:10.1016/s0960-894x(03)00386-x
PMID:12798324
Abstract

A series of aryltropane-based bivalent ligands was prepared and investigated for binding potency and for their ability to inhibit reuptake of human dopamine, serotonin and norepinephrine transporters. The bivalent ligand 4, comprised of linking an aryltropane by an octamethylene spacer showed high efficacy for the human dopamine transporter and had a discrimination ratio of 130.

摘要

制备了一系列基于芳基托烷的二价配体，并研究了它们的结合效力以及抑制人多巴胺、5-羟色胺和去甲肾上腺素转运体再摄取的能力。由八亚甲基间隔基连接芳基托烷组成的二价配体4对人多巴胺转运体显示出高效力，区分率为130。

相似文献

1
Bivalent biogenic amine reuptake inhibitors.二价生物胺再摄取抑制剂
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2
Biaryl analogues of conformationally constrained tricyclic tropanes as potent and selective norepinephrine reuptake inhibitors: synthesis and evaluation of their uptake inhibition at monoamine transporter sites.构象受限三环托烷的联芳基类似物作为强效和选择性去甲肾上腺素再摄取抑制剂：其在单胺转运蛋白位点的摄取抑制作用的合成与评价
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引用本文的文献

1
Bivalent phenethylamines as novel dopamine transporter inhibitors: evidence for multiple substrate-binding sites in a single transporter.双价苯乙胺类作为新型多巴胺转运体抑制剂：单一转运体中存在多个底物结合位点的证据。
J Neurochem. 2010 Mar;112(6):1605-18. doi: 10.1111/j.1471-4159.2010.06583.x. Epub 2010 Jan 12.
2
The synthesis of bivalent 2beta-carbomethoxy-3beta-(3,4-dichlorophenyl)-8-heterobicyclo[3.2.1]octanes as probes for proximal binding sites on the dopamine and serotonin transporters.合成二价2β-甲氧羰基-3β-(3,4-二氯苯基)-8-杂双环[3.2.1]辛烷作为多巴胺和5-羟色胺转运体上近端结合位点的探针。
Bioorg Med Chem. 2008 Feb 15;16(4):1832-41. doi: 10.1016/j.bmc.2007.11.009. Epub 2007 Nov 6.