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| 1 | Novel ^(99m)Tc labeled σ r eceptor ligand as a potential tumorimaging agent显示文摘A novel 99mTc labeled complex, [N-[2-((2-oxo-2-(4-(3-phenylpropyl)piperazin-1-yl)ethyl) (2-mercaptoethyl)amino)acetyl]-2-aminoethanethiolato]Technetium(V) oxide (PPPE-MAMA′-99mTcO) ([99mTc]-2) has been designed and prepared based on the integrated approach. The corresponding rhenium complex (PPPE-MAMA′-ReO)(Re-2) has been prepared and characterized. In vitro competi-tion binding assays show moderate affinity of Re-2 towards σ1 and σ2 receptors with Ki values of 8.67 ± 0.07 and 5.71 ± 1.88 μmol, respectively. Planar images obtained at 0.5 h, 4 h, 20 h after i.v. in-jection indicate the accumulation of [99mTc]-2 in MCF-7 human breast tumor bearing mice at 20 h. Furthermore, the accumulation of [99mTc]-2 has been inhibited at 20 h after co-injection of [99mTc]-2 plus haloperidol (1 mg/kg). Biodistribution studies of [99mTc]-2 display an in vivo tumor uptake of 0.14% ± 0.01% ID/g at 24 h post i.v. injection with a tumor/muscle ratio of 6.02 ± 0.87. The above results suggest that [99mTc]-2, derived from a previously published lead compound, retains certain tumor uptake and affinity for σ receptors. [99mTc]-2 may be used as a basis for further structural modifications to develop tumor imaging agents with high affinity for σ receptors. | FAN Caiyun1, JIA Hongmei1, Deuther-Conrad Winnie2, Brust Peter2, Steinbach J?rg2 & LIU Boli1 1. Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, Department of Chemistry, Beijing Normal University, Beijing 100875, China 2. Institute of Interdisciplinary Isotope Research, Permoserstr. 15, 04318 Leipzig, Germany Correspondence should be addressed to Liu Boli | 2006 | Science China Chemistry2006，49，2： | 2 |
| 2 | 显示文摘 | 张连启.? 医院电子档案的管理与利用措施分析(J)华章. 2013 (15) | 2013 | 华章2013，，： | 1 |
| 3 | 显示文摘 | 许进 高飞.? 浅论建筑施工管理技术(J)华章. 2011 (15) | 2011 | 华章2011，，15： | 1 |
| 4 | 显示文摘 | 华弘波.? 小说《镜花缘》中女性形象探析(J)华章. 2012 (15) | 2012 | 华章2012，，15： | 1 |
| 5 | NCLX protein, but not LETM1, mediates mitochondrial Ca^2+ extrusion, thereby limiting Ca^2+ -induced NAD(P) H production and modulating matrix redox state显示文摘 | De Marchi 15 Santo-Domingo J Castelbou C | 2014 | J Biol Chem2014，289，20： | 1 |
| 6 | 显示文摘 | 邓丽.? 旅游规划的环境影响识别研究(J)华章. 2014 (15) | 2014 | 华章2014，，15： | 1 |
| 7 | Diffusion-weighted magnetic resonance imaging for the detection of lipid-rich necrotic core in carot- id atheroma in vivo显示文摘 | Young VE Patterson A J Sadat 15 | 2010 | Neuroradiology2010，52，10： | 1 |
| 8 | 显示文摘 | 高婉芬.? CAD课程教学改革的研究与实践(J)华章. 2013 (15) | 2013 | 华章2013，，15： | 1 |
| 9 | 显示文摘 | 曲智威 牛彤 贾宝洋.? 红景天甙抗肝纤维化的实验研究(J)中华实用中西医杂志. 2004 (15) | 2004 | 中华实用中西医杂志2004，，： | 1 |
| 10 | 显示文摘 | Am J Respir FASEB J 2001 15 Bellini A Mattoli S | 2007 | Lab Invest2007，87，9： | 1 |
| 11 | Experimental investigation of cryogenic oscillating heat pipes 显示文摘 | JIAO A J MA H 15 CRITSER J K | 2009 | International Journal of Heat and Mass Transfer2009，52，1516： | 1 |
| 12 | 显示文摘 | 李雅杰.? 高频彩色多普勒超声综合指标诊断乳腺肿块的价值分析(J)中华现代临床医学杂志. 2005 (15) | 2005 | 中华现代临床医学杂志2005，，： | 1 |
| 13 | 显示文摘 | 刘晓远.? 关于《出纳岗位实务》课程的几点思考(J)华章. 2012 (15) | 2012 | 华章2012，，15： | 1 |
| 14 | Risk ot myocandinl iniarctionand vascular death after transient ischemic attack and ischemicstmke: a systematic review and meta- analysis显示文摘 | J touze E V arenne 12hatelliter 15 | 2005 | Stroke2005，36，12： | 1 |
| 15 | Renin increases mesangi& B, and m&trix proteins through receptor- mech&nisms显示文摘 | Huang Y Wongamorntham cell tr&nsforming growth f&ctor medi&ted angiotensin II-independent ]15 $ Kasting J et &l | 2006 | Kidney Int2006，69，1： | 1 |
| 16 | 显示文摘 | 尹领巧 高红欣.? 高职实践教学质量评价体系研究(J)华章. 2014 (15) | 2014 | 华章2014，，15： | 1 |
| 17 | 显示文摘 | 刘翠祥.? 如何让中学语文课堂变得有活力(J)现代阅读(教育版). 2011 (15) | 2011 | 现代阅读(教育版)2011，，15： | 1 |
| 18 | The Ettects ot Boron Addi- tions on the Oxidation Behavior of Carbon显示文摘 | Mckee DW 5plro 15 L Lamby E J | 1984 | Carbon1984，22，6： | 1 |
| 19 | 显示文摘 | 赵莉萍 鲍群.? 老年患者的心理护理(J)中华实用中西医杂志. 2005 (15) | 2005 | 中华实用中西医杂志2005，，15： | 1 |
| 20 | 显示文摘 | 黎玉康.? 城乡义务教育均衡发展的关键是提高农村小学教师的素质(J)现代阅读(教育版). 2010 (15) | 2010 | 现代阅读(教育版)2010，，15： | 1 |
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