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Radiosynthesis of a novel potential adenosine A3 receptor ligand, 5-ethyl 2,4-diethyl-3-((2-[18F]fluoroethyl)sulfanylcarbonyl)-6-phenylpyridine-5-carboxylate ([18F]FE@SUPPY:2) 新型潜在腺苷A3受体配体5-乙基2,4-二乙基-3-((2-[18F]氟乙基)磺酰基羰基)-6-苯基吡啶-5-羧酸盐([18F]FE@SUPPY:2)的放射性合成
Pub Date : 2009-12-01 DOI: 10.1524/RACT.2009.1663
D. Haeusler, M. Mitterhauser, L. Mien, K. Shanab, R. Lanzenberger, E. Schirmer, J. Ungersboeck, L. Nics, H. Spreitzer, H. Viernstein, R. Dudczak, et al.
Abstract Since, to date very limited information on the distribution and function of the adenosine A3 receptor is available, the development of suitable radioligands is needed. Recently, we introduced [ 18F]FE@SUPPY (5-(2-[ 18F]fluoroethyl) 2,4-diethyl-3-(ethylsulfanylcarbonyl)-6-phenylpyridine-5-carboxylate) as the first PET-ligand for the A3R. Regarding the metabolic profile – this class of dialkylpyridines comprises two ester functions within one molecule, one carboxylic and one thiocarboxylic – one could expect carboxylesterases significantly contributing to cleavage and degradation. Therefore, our aim was the development of [ 18F]FE@SUPPY:2 (5-ethyl 2,4-diethyl-3-((2-[ 18F]fluoroethyl)sulfanylcarbonyl)-6-phenylpyridine-5-carboxylate), the functional isomer containing the label at the thiocarboxylic moiety. For satisfactory yields in high scale radiosyntheses, a reaction temperature of 75 °C has to be applied for at least 20 min using 20 mg/mL of precursor. So far, 6 complete high-scale radiosyntheses were performed. Starting from an average of 51.2±21.8 GBq (mean±SD) [ 18F]fluoride, 5.8±4.1 GBq of formulated [ 18F]FE@SUPPY:2 (12.0±5.4%, based on [ 18F]fluoride, not corrected for decay) were prepared in 75±8 min.
由于迄今为止关于腺苷A3受体的分布和功能的信息非常有限,因此需要开发合适的放射性配体。最近,我们引入了[18F]FE@SUPPY (5-(2-[18F]氟乙基)2,4-二乙基-3-(乙基磺酰基羰基)-6-苯基吡啶-5-羧酸盐)作为A3R的第一个pet配体。关于代谢谱-这类二烷基吡啶在一个分子内包含两个酯功能,一个羧基和一个硫羧基-可以预期羧基酯酶对裂解和降解有重要作用。因此,我们的目标是开发[18F]FE@SUPPY:2(5-乙基2,4-二乙基-3-((2-[18F]氟乙基)磺酰基羰基)-6-苯基吡啶-5-羧酸盐),这是一种功能异构体,在硫羧基部分含有标签。为了在大规模放射性合成中获得满意的产率,必须使用20mg /mL前体,在75°C的反应温度下应用至少20分钟。到目前为止,进行了6次完整的大规模放射性合成。从平均51.2±21.8 GBq (mean±SD) [18F]氟化物开始,在75±8分钟内制备了5.8±4.1 GBq的配方[18F]FE@SUPPY:2(12.0±5.4%,基于[18F]氟化物,未校正衰变)。
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引用次数: 5
Separation of 109Cd from silver targets by nanohematite 纳米赤铁矿从银靶中分离109Cd
Pub Date : 2009-12-01 DOI: 10.1524/RACT.2009.1664
M. Sadeghi, H. Karami, P. Sarabandi, M. Mirzaee
Abstract 109Cd was produced at a cyclotron vianatAg(p, n) 109Cd reaction by irradiation of an electroplated target with 15 MeV protons. The obtained yield was 70 kBq/μA h. The separation was performed using hematite nano-particles as sorbent which were synthesized by a solid-state chemical reaction method. The effect of different parameters, such as pH and the sorbent concentration, on extraction efficiency were investigated. The phase morphology, nanostructure and size of nano-particles were studied by X-ray diffraction (XRD) and scanning electron microscopy (SEM). The chemical and radionuclidic purity of 109Cd was determined by ICP-AES and HPGe detector gamma-ray spectrometry, respectively.
摘要以15mev质子辐照电镀靶,利用回旋加速器vianatAg(p, n) 109Cd反应制备了109Cd。所得收率为70 kBq/μA h。采用固相化学反应法制备纳米赤铁矿作为吸附剂进行分离。考察了pH、吸附剂浓度等参数对萃取效率的影响。采用x射线衍射(XRD)和扫描电镜(SEM)研究了纳米颗粒的相形态、纳米结构和尺寸。采用ICP-AES和HPGe探测器γ -能谱法分别测定了109Cd的化学纯度和放射性同位素纯度。
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引用次数: 7
Charged particle induced reaction cross section data for production of the emerging medically important positron emitter 64Cu: A comprehensive evaluation 新型医学上重要的正电子发射器64Cu的带电粒子诱导反应截面数据的综合评价
Pub Date : 2009-12-01 DOI: 10.1524/RACT.2009.1670
M. Aslam, S. Sudár, M. Hussain, A. A. Malik, H. Shah, S. Qaim
Abstract The radionuclide 64Cu (T1/2=12.7 h) is an important non-standard positron emitter, suitable for combining PET imaging and targeted therapy. Its production in no-carrier-added form is done via charged particle induced reactions, and considerable amount of cross section data are available in the literature. We evaluated seven reactions, namely 64Ni(p, n) 64Cu, 64Ni(d, 2n) 64Cu, 68Zn(p, αn) 64Cu, 66Zn(p, 2n) 64Cu, 64Zn(d, 2p) 64Cu, 66Zn(p, α) 64Cu and natZn(d, x) 64Cu. Data analysis was generally limited up to about 25 MeV and the consistency check of experimental data was carried out using the nuclear model codes STAPRE, EMPIRE and TALYS. In a few cases experimental data were available up to 100 MeV; the consistency check in the high energy region was done only using the code TALYS. A statistical procedure (supported by nuclear model calculations) was then used to fit the data. The derived recommended sets of data, together with 95% confidence limits, are reported. The integral yields calculated from those data are also given. A critical comparison of the various production routes of 64Cu is presented. The 64Ni(p, n) 64Cu reaction, utilizing a highly enriched target, is the method of choice.
放射性核素64Cu (T1/2=12.7 h)是一种重要的非标准正电子发射器,适用于PET成像与靶向治疗相结合。其无载流子添加形式的生产是通过带电粒子诱导反应完成的,并且在文献中有相当数量的截面数据。我们评价了64Ni(p, n) 64Cu、64Ni(d, 2n) 64Cu、68Zn(p, αn) 64Cu、66Zn(p, 2n) 64Cu、64Zn(d, 2p) 64Cu、66Zn(p, α) 64Cu和natZn(d, x) 64Cu 7种反应。数据分析一般限制在25 MeV左右,实验数据的一致性检查使用核模型代码STAPRE、EMPIRE和TALYS进行。在少数情况下,实验数据高达100兆电子伏特;在高能区域的一致性检查只使用代码TALYS完成。然后使用统计程序(由核模型计算支持)来拟合数据。报告了导出的推荐数据集以及95%的置信限。并给出了用这些数据计算的积分产率。对不同的64Cu生产工艺进行了比较。采用高富集靶的64Ni(p, n) 64Cu反应是首选方法。
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引用次数: 42
Investigation of K to L shell/subshell vacancy transitions of Zn and Fe in FexZn1-x thin film alloys FexZn1-x薄膜合金中Zn和Fe的K到L壳层/亚壳层空位跃迁研究
Pub Date : 2009-12-01 DOI: 10.1524/RACT.2009.1662
Ö. Söğüt
Abstract The vacancy transfer probabilities from K-shell to L2-, L3- and L-shell/subshells were measured in FexZn1-x thin film alloys. The samples were excited by γ photons with energy 59.5 keV from a 50 mCi 241Am radioisotope source. The emitted K X-rays were detected by an Ultra-LEGe having a resolution of 150 eV at 5.9 keV. For comparison with experimental results, theoretical calculations have been made using radiative and nonradiative transition rates. The measured results are in good agreement with theoretically calculated values within experimental errors. FexZn1-x thin film alloys were electrochemically deposited on aluminum substrates from sulfate bath. In conclusion, it was found that the vacancy transfer probabilities changed in FexZn1-x thin films for different compositions of x.
摘要测量了FexZn1-x薄膜合金中k壳层向L2-、L3-和l壳层/亚壳层的空位转移概率。样品被来自50mci 241Am放射性同位素源的能量为59.5 keV的γ光子激发。发射的K x射线由分辨率为150 eV, 5.9 keV的Ultra-LEGe检测到。为了与实验结果进行比较,用辐射和非辐射跃迁速率进行了理论计算。测量结果与理论计算值在实验误差范围内吻合较好。采用硫酸盐浴法制备了FexZn1-x薄膜合金。综上所述,在不同的x组分下,FexZn1-x薄膜中的空位转移概率发生了变化。
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引用次数: 2
期刊
Radiochimica Acta Radiochimica Acta
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