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| 1 | Development of ^(18)F-labeled radiotracers for neuroreceptor imaging with positron emission tomography显示文摘Positron emission tomography(PET)is an in vivo molecular imaging tool which is widely used in nuclear medicine for early diagnosis and treatment follow-up of many brain diseases.PET uses biomolecules as probes which are labeled with radionuclides of short half-lives,synthesized prior to the imaging studies.These probes are called radiotracers.Fluorine-18 is a radionuclide routinely used in the radiolabeling of neuroreceptor ligands for PET because of its favorable half-life of 109.8 min.The delivery of such radiotracers into the brain provides images of transport,metabolic,and neurotransmission processes on the molecular level.After a short introduction into the principles of PET,this review mainly focuses on the strategy of radiotracer development bridging from basic science to biomedical application.Successful radiotracer design as described here provides molecular probes which not only are useful for imaging of human brain diseases,but also allow molecular neuroreceptor imaging studies in various small-animal models of disease,including geneticallyengineered animals.Furthermore,they provide a powerful tool for in vivo pharmacology during the process of pre-clinical drug development to identify new drug targets,to investigate pathophysiology,to discover potential drug candidates,and to evaluate the pharmacokinetics and pharmacodynamics of drugs in vivo. | Peter Brust Jrg van den Hoff Jrg Steinbach | 2014 | Neuroscience Bulletin2014，30，5： | 3 |
| 2 | 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 |
| 3 | Reflective and black mulch increase yield in pumpkins under virus disease pressure显示文摘 | Brust G E | 2000 | Journal of Economic Entomology2000，93，： | 1 |
| 4 | Neurologic aspects of cobalamin deficiency 显示文摘 | Healton EB Savage DG Brust JCM | 1991 | Medicine1991，70，： | 1 |
| 5 | Preparation of acrylate-stabilized gold and silver hydrosols and gold polymer composite films显示文摘 | HUSSAIN I BRUST M PAPWORTH A J | 2003 | Langmuir2003，19，： | 1 |
| 6 | Validity of the depression coping self-efficacy scale 显示文摘 | Tucker S Brust S Richardson B | 2002 | Arch Psychiatr Nuts2002，16，3： | 1 |
| 7 | A computational model of backlaywelding for controlling residual stresses welded pipes显示文摘 | Brust F W Rybicki E F | 1981 | Transactions of ASMEJournal of Pressure Vessel Technology1981，103，： | 1 |
| 8 | Neurologic aspects of cobalamin deficiency 显示文摘 | Healton EB Savage DG Brust JC | 1991 | Medicine(Baltimore)1991，70，： | 1 |
| 9 | 新的^(99m)Tc标记σ受体肿瘤显像剂显示文摘采用整体法设计合成了新的99mTc标记的配合物[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)及其相应的铼配合物(PPPE-MAMA′-ReO)(Re-2).竞争结合实验表明Re-2对σ1和σ2受体有中等亲和力,Ki值分别为8.67±0.07和5.71±1.88μmol/L;荷MCF-7人乳癌裸鼠尾静脉注射[99mTc]-2后0.5h,4h,20h采集平面图像,20h时可以看到肿瘤部位有放射性浓集,共同注射[99mTc]-2和抑制剂氟哌啶醇(1mg/kg)后显像,20h时肿瘤部位无明显放射性浓集;体内生物分布结果显示,注射后24h肿瘤中的放射性摄取为0.14%±0.01%ID/g,肿瘤/肌肉比为6.02±0.87.上述结果表明:虽然用整体设计法对前体化合物的结构进行了较大修饰,但得到的99mTc-配合物([99mTc]-2)在肿瘤内仍有一定的浓集,与σ1和σ2受体仍保持一定的亲和力.在此配合物的基础上,对其进行进一步的结构修饰有可能得到对σ受体亲和力更高的肿瘤显像剂. | 樊彩云 贾红梅 Deuther-Conrad Winnie Brust Peter Steinbach Jrg 刘伯里 | 2005 | 中国科学(B辑)2005，35，6： | 1 |
| 10 | Expression of the lacZ gene from two methanol-regulated promoters in Pichia pastoris显示文摘 | BRUST P F CREGG J M | 1987 | Nucleic Acid Res1987，15，9： | 1 |
| 11 | 17-hydroxylation deficiency in man显示文摘 | Biglieri EG Herron MA Brust N | 1966 | J Clin Invest1966，45，12： | 1 |
| 12 | Some Recent Advances in Nanostructure Preparation from Gold and Silver Particles: a Short Topical Review显示文摘 | Brust M Kiley C J | 2002 | Colloids Surf a Physicochem Eng Aspects2002，202，： | 1 |
| 13 | Neurologic aspects of cobalamin deficiency显示文摘 | Heahon EB SavageDG Brust JCM etal | 1991 | Medicine1991，70，： | 1 |
| 14 | Acute venntricular hemorrhage in adults with hydrocephalus managed by corpus callosotomy and fenestration of the septumm pellucidum显示文摘 | Holtzman RN Brust JC Ainyette IG | 2001 | J Neurosurg2001，95，1： | 1 |
| 15 | Welding Residual Stresses and Effects of Fracture in Pressure Vessel and Piping Components:A Millennium Review and Beyond显示文摘 | DONG P BRUST F W | 2000 | Journal of Pressure Vessel Technology2000，122，3： | 1 |
| 16 | Acute ventricular hemorrhage in adults with hydrocephalus managed by coipus callosotomy and fenestration of the septum peilucidum显示文摘 | Holtzman PN Brust JC Ainyette IG | 2011 | Neurosurg2011，95，1： | 1 |
| 17 | A computational model of backlay welding for controlling residual stresses in welded pipes 显示文摘 | Brust F W Rybicki E F | 1981 | Transactions of ASME Journal of Pressure Vessel Technology1981，103，： | 1 |
| 18 | Acute ventricular hemorrhage in adults with hydrocephalus managed by corpus callosotomy and fenestration of the septum pellucidum显示文摘 | Holtzman RNN Brust JCM Bowers PP | 2001 | Neurosurgery2001，95，： | 1 |
| 19 | Crack-opening-area analyses for circumferen-tial through-wall cracks in pipes,Part I : Ana-lytical models显示文摘 | RAHMAN S BRUST F W GHADIALI N etal | 1998 | International Journal of Pres-sure Vessels and Piping1998，75，5： | 1 |
| 20 | Preparation ofacrylate-stabilized gold and silver hydrosols and goldpolymercomposite films显示文摘 | HUSSAIN I BRUST M PAPWORTH A J | 2003 | Langmuir2003，19，11： | 1 |
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