北京大学医学部机构知识库
Advanced  
IR@PKUHSC  > 北京大学药学院  > 药剂学系  > 期刊论文
学科主题: 药学
题名:
Novel Cyclopentadienyl Tricarbonyl Tc-99m Complexes Containing 1-Piperonylpiperazine Moiety: Potential Imaging Probes for Sigma-1 Receptors
作者: Wang, Xia1; Li, Dan1; Deuther-Conrad, Winnie2; Lu, Jie1; Xie, Ying3; Jia, Bing4; Cui, Mengchao1; Steinbach, Joerg2; Brust, Peter2; Liu, Boli1; Jia, Hongmei1
刊名: JOURNAL OF MEDICINAL CHEMISTRY
发表日期: 2014-08-28
DOI: 10.1021/jm5009488
卷: 57, 期:16, 页:7113-7125
收录类别: SCI ; IC
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: POSITRON-EMISSION-TOMOGRAPHY ; BIOLOGICAL EVALUATION ; DOPAMINE TRANSPORTER ; ALZHEIMERS-DISEASE ; HIGH OCCUPANCY ; HUMAN BRAIN ; IN-VITRO ; LIGANDS ; BINDING ; AGENTS
英文摘要:

We report the design, synthesis, and evaluation of a series of novel cyclopentadienyl tricarbonyl Tc-99m complexes as potent sigma(1) receptor radioligands. Rhenium compounds 3-(4-(1,3-benzodioxol-5-ylmethyl)piperazin-1-yl)propylcarbonylcyclopentadienyl tricarbonyl rhenium (10a) and 4-(4-(1,3-benzodioxol-5-ylmethyl)piperazin-1-yl)butylcarbonylcyclopentadienyl tricarbonyl rhenium (10b) possessed high in vitro affinity for sigma(1) receptors and moderate to high selectivity for sigma(2) receptors and the vesicular acetylcholine transporter. Biodistribution studies in mice demonstrated high initial brain uptake for corresponding Tc-99m derivatives [Tc-99m] 23 and [Tc-99m]24 of 2.94 and 2.13% injected dose (ID)/g, respectively, at 2 min postinjection. Pretreatment of haloperidol significantly reduced the radiotracer accumulation of [Tc-99m]23 or [Tc-99m]24 in the brain. Studies of the cellular uptake of [Tc-99m]23 in C6 and DU145 tumor cells demonstrated a reduction of accumulation by incubation with haloperidol, 1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine (SA4503), or 1,3-di-o-tolyl-guanidine (DTG). Furthermore, blocking studies in C6 glioma-bearing mice confirmed the specific binding of [Tc-99m]23 to sigma(1) receptors in the tumor.

语种: 英语
所属项目编号: 21071023
项目资助者: National Natural Science Foundation of China
WOS记录号: WOS:000341121400017
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/54595
Appears in Collections:北京大学药学院_药剂学系_期刊论文

Files in This Item:

There are no files associated with this item.


作者单位: 1.Beijing Normal Univ, Coll Chem, Minist Educ, Key Lab Radiopharmaceut, Beijing 100875, Peoples R China
2.Helmholtz Zentrum Dresden Rossendorf, Dept Neuroradiopharmaceut, Inst Radiopharmaceut Canc Res, D-04318 Leipzig, Germany
3.Peking Univ, Sch Pharmaceut Sci, Dept Pharmaceut, Beijing 100191, Peoples R China
4.Peking Univ, Sch Basic Med Sci, Dept Radiat Med, Beijing 100191, Peoples R China

Recommended Citation:
Wang, Xia,Li, Dan,Deuther-Conrad, Winnie,et al. Novel Cyclopentadienyl Tricarbonyl Tc-99m Complexes Containing 1-Piperonylpiperazine Moiety: Potential Imaging Probes for Sigma-1 Receptors[J]. JOURNAL OF MEDICINAL CHEMISTRY,2014,57(16):7113-7125.
Service
Recommend this item
Sava as my favorate item
Show this item's statistics
Export Endnote File
Google Scholar
Similar articles in Google Scholar
[Wang, Xia]'s Articles
[Li, Dan]'s Articles
[Deuther-Conrad, Winnie]'s Articles
CSDL cross search
Similar articles in CSDL Cross Search
[Wang, Xia]‘s Articles
[Li, Dan]‘s Articles
[Deuther-Conrad, Winnie]‘s Articles
Related Copyright Policies
Null
Social Bookmarking
Add to CiteULike Add to Connotea Add to Del.icio.us Add to Digg Add to Reddit

Items in IR are protected by copyright, with all rights reserved, unless otherwise indicated.

 

 

Valid XHTML 1.0!
Copyright © 2007-2017  北京大学医学部 - Feedback
Powered by CSpace