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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 | Analysis of intraoperative rupture in the surgical treatment of 1694 saccular anemysms 显示文摘 | Leipzig TJ Morgan J Homer TG | 2005 | Neurosurgery2005，56，3： | 1 |
| 3 | Role of intraoperative angiography in the surgical treatment of cerebral aneurysms显示文摘 | Payner TD Horner TG Leipzig TJ | 1998 | J Neurosurg1998，88，： | 1 |
| 4 | Functional evaluation of the spinal accessory nerve after neck dissection 显示文摘 | Leipzig B Suen JY English JL | 1983 | Am J Surg1983，146，5： | 1 |
| 5 | Analysis of intraoperative rupture in the surgical treatment of 1694 saecular aneurysms 显示文摘 | Leipzig TJ Morgan J Homer TG | 2005 | Neurosurgery2005，56，3： | 1 |
| 6 | Analysis of intraoperative rupture in the surgical treatment of 1694 saccular aneurysms显示文摘 | Leipzig TJ Morgan J Homer TG | 2005 | Neurosurgery2005，56，3： | 1 |
| 7 | Acute cauda equina syndrome compression显示文摘 | Coscia M Leipzig T Cooper D | 1994 | Spine1994，19，： | 1 |
| 8 | Functional evaluation of the spinal accessory nerve after neck dissection显示文摘 | Leipzig B Suen JY English JL | 1983 | Am J Surg1983，146，： | 1 |
| 9 | A multicenter,pro-spective,randomized trial evaluating a new hemostatic agent for spinal surgery显示文摘 | Renkens KL Jr Payner TD Leipzig TJ | 2001 | Spine2001，26，15： | 1 |
| 10 | A multicenter, pro- spective, randomized trial evaluating a new hemostatic agent for spinal surgery显示文摘 | Renkens KL Jr Payner TD Leipzig TJ | 2001 | Spine2001，26，15： | 1 |
| 11 | The Future of Pension Reform in Latin America显示文摘 | De Ferranti D Leipziger D Srinivas P S | 2002 | Finance and Development2002，，3： | 1 |
| 12 | Role of intraoperative angiography in the surgical treatment of cerebral aneurysms显示文摘 | Horner TG Leipzig TJ | 1998 | J Neurosurg1998，88，： | 1 |
| 13 | Analysis of intraoperative rupture in the surgical treatment of 1694 saecuIar aneurysms 显示文摘 | Leipzig TJ Morgan J Homer TG | 2005 | Neurosurgery2005，56，3： | 1 |
| 14 | Functional immobilization of interferon-gamma induces neuronal differentiation of neural stem cells显示文摘 | Leipzig N D Xu C Zahir T | 2010 | J Biomed Mater Res A2010，93，2： | 1 |
| 15 | Analysis of intra- operative rupture in the surgical treatment of 1694 saccular aneurysms 显示文摘 | Leipzig T J Morgan J Homer TG | 2005 | Neurosurgery2005，56，3： | 1 |
| 16 | Congenital cerebrospianl otorrhea显示文摘 | Gacek RR Leipzig B | 1979 | Ann Otol1979，88，： | 1 |
| 17 | Patient - initiated device removal in intensive care units: A national prevalence study显示文摘 | Mion LC Minnick AF Leipzig RM | 2010 | Crit care Meal2010，35，： | 1 |
| 18 | Analysis of intra-operative rupture in the surgical treatment of 1 694 saccular aneurysms 显示文摘 | Leipzig TJ Morgan J Horner TG | 2005 | Neurosurgery2005，56，： | 1 |
| 19 | DNA bar coding and pyrosequencing to identify rare HIV drug resistance mutations 显示文摘 | Hoffmann C Minkah N Leipzig J | 2007 | Nucleic Acids Res2007，35，13： | 1 |
| 20 | The effect of substrate stiffness on adult neural stem cell behavior显示文摘 | Leipzig N D Shoichet M S | | 0，，36： | 1 |
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