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一系列托烷类似物作为新型囊泡单胺转运体-2配体的合成与评价

Synthesis and evaluation of a series of tropane analogues as novel vesicular monoamine transporter-2 ligands.

作者信息

Zheng Guangrong, Dwoskin Linda P, Deaciuc Agripina G, Crooks Peter A

机构信息

College of Pharmacy, University of Kentucky, Lexington, KY 40536-0082, USA.

出版信息

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4463-6. doi: 10.1016/j.bmcl.2005.07.032.

DOI:10.1016/j.bmcl.2005.07.032
PMID:16112864
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3602420/
Abstract

A series of tropane derivatives has been synthesized as lobelane analogues and evaluated for their binding affinity at the vesicular monoamine transporter-2 (VMAT2), and at alpha4beta2* and alpha7* nicotinic acetylcholine receptors. The trop-2-ene analogues 4a and 4b exhibited good affinity and high selectivity for VMAT2.

摘要

已经合成了一系列托烷衍生物作为洛贝林类似物，并评估了它们对囊泡单胺转运体-2（VMAT2）以及α4β2和α7烟碱型乙酰胆碱受体的结合亲和力。托品-2-烯类似物4a和4b对VMAT2表现出良好的亲和力和高选择性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c3bb/3602420/0b5b6fca4810/nihms446066f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c3bb/3602420/44c58fdfbfe3/nihms446066f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c3bb/3602420/0b5b6fca4810/nihms446066f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c3bb/3602420/44c58fdfbfe3/nihms446066f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c3bb/3602420/0b5b6fca4810/nihms446066f2.jpg

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本文引用的文献

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Lobelane analogues as novel ligands for the vesicular monoamine transporter-2.洛贝林类似物作为囊泡单胺转运体-2的新型配体。
Bioorg Med Chem. 2005 Jun 2;13(12):3899-909. doi: 10.1016/j.bmc.2005.04.013.
2
Lobeline analogs with enhanced affinity and selectivity for plasmalemma and vesicular monoamine transporters.对质膜和囊泡单胺转运体具有增强亲和力和选择性的洛贝林类似物。
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Two isomers of 2,4-dibenzyl-8-azabicyclo[3.2.1]octan-3-ol.2,4-二苄基-8-氮杂双环[3.2.1]辛烷-3-醇的两种异构体。
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2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.2002年药物化学分部奖致辞：单胺转运体与阿片受体。成瘾治疗的靶点。
J Med Chem. 2003 May 8;46(10):1775-94. doi: 10.1021/jm030092d.
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Brain reward circuitry: insights from unsensed incentives.大脑奖赏回路：来自未察觉激励的见解。
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Probes for the dopamine transporter: new leads toward a cocaine-abuse therapeutic--A focus on analogues of benztropine and rimcazole.多巴胺转运体探针：可卡因成瘾治疗的新线索——聚焦苯海索和利米唑类似物
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The Interactions of the 5-HT(3) receptor with arylpiperazine, tropane, and quinuclidine ligands.5-羟色胺（3）受体与芳基哌嗪、托烷和奎宁环配体的相互作用。
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A novel mechanism of action and potential use for lobeline as a treatment for psychostimulant abuse.洛贝林作为治疗精神兴奋剂滥用的一种新作用机制及潜在用途。
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