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Novel Cyclopentadienyl Tricarbonyl Tc-99m Complexes Containing 1-Piperonylpiperazine Moiety: Potential Imaging Probes for Sigma-1 Receptors
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
2014-08-28
DOI10.1021/jm5009488
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
WOS记录号WOS:000341121400017
项目编号21071023
资助机构National Natural Science Foundation of China
引用统计
被引频次:11[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/54595
专题北京大学药学院_药剂学系
北京大学基础医学院
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
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GB/T 7714
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.
APA Wang, Xia.,Li, Dan.,Deuther-Conrad, Winnie.,Lu, Jie.,Xie, Ying.,...&Jia, Hongmei.(2014).Novel Cyclopentadienyl Tricarbonyl Tc-99m Complexes Containing 1-Piperonylpiperazine Moiety: Potential Imaging Probes for Sigma-1 Receptors.JOURNAL OF MEDICINAL CHEMISTRY,57(16),7113-7125.
MLA Wang, Xia,et al."Novel Cyclopentadienyl Tricarbonyl Tc-99m Complexes Containing 1-Piperonylpiperazine Moiety: Potential Imaging Probes for Sigma-1 Receptors".JOURNAL OF MEDICINAL CHEMISTRY 57.16(2014):7113-7125.
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