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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 | Involvement of serum retinoids and Leiden mutation in patients with esophageal, gastric, liver, pancreatic, and colorectal cancers in Hungary显示文摘AIM: To analyze the serum levels of retinoids and Leiden mutation in patients with esophageal, gastric, liver,pancreatic, and colorectal cancers.METHODS: The changes in serum levels of retinoids (vitamin A, α- and β-carotene, α- and β-cryptoxanthin,zeaxanthin, lutein) and Leiden mutation were measured by high liquid performance chromatography (HPLC)and polymerase chain reaction (PCR) in 107 patients (70 males/37 females) with esophageal (0/8), gastric (16/5), liver (8/7), pancreatic (6/4), and colorectal (30/21including 9 patients suffering from in situ colon cancer)cancer. Fifty-seven healthy subjects (in matched groups)for controls of serum retinoids and 600 healthy blood donors for Leiden mutation were used.RESULTS: The serum levels of vitamin A and zeaxanthin were decreased significantly in all groups of patients with gastrointestinal (GI) tumors except for vitamin A in patients with pancreatic cancer. No changes were obtained in the serum levels of α- and β-carotene,α- and β-cryptoxanthin, zeaxanthin, lutein in patients with GI cancer. The prevalence of Leiden mutation significantly increased in all groups of patients with GI cancer.CONCLUSION: Retinoids (as environmental factors)are decreased significantly with increased prevalence of Leiden mutation (as a genetic factor) in patients before the clinical manifestation of histologically different (planocellular and hepatocellular carcinoma, and adenocarcinoma) GI cancer. | Gyula Mózsik Gy(o|¨)rgy Rumi András D(o|¨)m(o|¨)t(o|¨)r Mária Figler Beáta Gasztonyi El(?)d Papp Alajos Pár Gabriella Pár József Belágyi Zoltán Matus Béla Melegh | 2005 | World Journal of Gastroenterology2005，11，48： | 2 |
| 3 | A review of metabolic and cardiovascular effects of oral antidiabetic agents:beyond glucose-level lowering显示文摘 | Plutzky J Sobel BE | 1999 | J Cardiovasc Risk1999，6，： | 1 |
| 4 | Evaluat ion of intracoro- nary stenting by intravascular optical coherence tomography 显示文摘 | Bouma BE Teamey C J Yabushita H et aI | 2003 | Heart2003，89，： | 1 |
| 5 | The relation between hip impact velocity and hip impact force differs between sideways fall techniques显示文摘 | Groen BE Weerdesteyn V Duysens J | 2008 | J Electromyogr Kineol2008，18，2： | 1 |
| 6 | Atmospheric transport of emissions from a motorway - measurement and modeling显示文摘 | Kuhler M Kraft J Beβ H | 1990 | The Science of The Total Environment1990，93，： | 1 |
| 7 | The American customer satisfaction index:nature,purpose,and findings显示文摘 | Fornell C Johnson MD Anderson EW Cha J Bryant BE | 1996 | The Journal of Mar_ket_ing1996，60，： | 1 |
| 8 | Reproducibility, fidelity, and discriminant validity of mRNA amplification for microarray analysis from primary hematopoietic ceils 显示文摘 | Li L Roden J Shapiro BE | 2005 | Mol Diagn2005，7，1： | 1 |
| 9 | Disappear anee of pink- pigmented Globigerinoides ruber at 120 000 yr B P in the Indian and Pacific Oceans 显示文摘 | Thompson P R Be A W H Duplesy J C | 1999 | Nature1999，280，： | 1 |
| 10 | Co-ocemTence of social anxiety and depression symptoms in adolescence:differential links with implicit and explicit self-esteem 显示文摘 | De Jong P J Sportel BE De Hullu E | 2012 | Psychol Med2012，42，3： | 1 |
| 11 | Fatty fish in the diet of patients with type 2 diabetes: comparison of the metabolic effects of foods rich in n-3 and n-6 fatty acids显示文摘 | Karlstr?m BE J?rvi AE Byberg L | 2011 | Am J Clin Nutr2011，94，1： | 1 |
| 12 | Review article : current treatment options and management of functional dyspepsia 显示文摘 | Lacy BE TaUey N J Locke GR | 2012 | Alimentary pharmacology & therapeutics2012，36，1： | 1 |
| 13 | Thmnfi)oelastometry: a contribution to perioperative free-flap management 显示文摘 | Wikner J Beck-Broichsitter BE Schlesinger S | 2015 | J Craniomaxillofac Surg2015，43，7： | 1 |
| 14 | Epidemiology of fracture of the upper end of the huumerus显示文摘 | Horak J Nilsson BE | 1975 | Clin Orthop1975，112，： | 1 |
| 15 | Elevated levels of homocysteine increase IL-6 production in monocytic Mono Mac 6 cells 显示文摘 | van Aken BE Jansen J van Deventer S J | 2000 | Blood Coagul Fibrinolysis2000，11，2： | 1 |
| 16 | Births: final data for 2001 显示文摘 | Martin JA Hamilton BE Ventura S J | 2002 | National Statistics Report2002，51，2： | 1 |
| 17 | Resistance to diet-induced obesity: food intake, pancreatic sympathetic tone, and insulin 显示文摘 | Levin BE Triscari J Hogan S | 1987 | Am J Physiol1987，252，32： | 1 |
| 18 | Motor unit number estimates in idiopathic Parkinson's disease显示文摘 | Caviness JN Smith BE Clarke Stevens J | 2002 | Parkinsonism Relat Disord2002，8，3： | 1 |
| 19 | Association of polymorphisms in microRNA machinery genes (DROSHA, DICER1, RAN, and XPO5) with risk of idiopathic primary ovarian insufficiency in Korean women显示文摘 | Rah H Jeon Y J Lee BE | 2013 | Menopause2013，20，10： | 1 |
| 20 | BirA En- zyme: Production and Application in the Study of Mem- brane Receptor - Ligand Interactions by Site-Specific Biotinylation Original Research 显示文摘 | O'Callaghan C A Byford M F Wyer J R Willcox BE Jakobsen B K McMichael A J Bell J 1 | 1999 | Anal Biochem1999，266，1： | 1 |
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