Synthesis,labelling and animal experiments of the derivative of phenylpentadecanoic acid（CACPPA）

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高Tc超导薄膜的实用化问题

本文叙述了高Te超导薄膜的主要进展,并讨论了它的实用化问题     

~(99)Tc~m-MPAQ的合成及其生物分布

为寻找新的^99Tc^m脑灌注显像剂，对^99Tc^m-MPBDA进行了结构修饰。在制备N-(2-巯基丙基)-1，2-苯二胺(MPBDA)基础上合成了三齿配体8-[N-(2-巯基丙基)]-氨基喹啉(MPAQ)，产物经IR，^1H NMR，MS及元素分析等表征确认。以氯离子为单齿配体，用直接标记法制备了^99Tc^m—MPAQ，确定了最佳标记条件，测定了标记物的稳定性和脂溶性。实验结果表明，^99Tc^m-MPAQ放化纯在96％以上，室温下在水溶液中稳定6h以上，脂溶性比^99Tc^m-MPBDA的大。生物分布试验结果表明，^99Tc—MPAQ生物性质没有^99Tc^m-MPBDA的好，但它可以穿过正常的血脑屏障，有-定的脑摄取(1．55％／g)和脑滞留(注射后30min仍有初始摄入量的62%).     

A novel high temperature superconducting magnetic flux pump for MRI magnets

This paper presents a kind of minitype magnetic flux pump made of high temperature superconductor. This kind of novel high temperature superconducting (HTS) flux pump has not any mechanical revolving parts or thermal switches. The excitation current of copper coils in magnetic pole system is controlled by a singlechip. The structure design and operational principle have been described. The operating performance of the new model magnetic flux pump has been preliminarily tested. The experiments show that the maximum pumping current is approximately 200 A for Bi2223 flux pump and 80 A for MgB₂ flux pump operating at 20 K. By comparison, it is discovered that the operating temperature range is wider, the ripple is smaller and the pumping frequency is higher in Bi2223 flux pump than those in MgB₂ flux pump. These results indicate that the newly developed Bi2223 magnetic flux pump may efficiently compensate the magnetic field decay in HTS magnet and make the magnet operate in persistent current mode, this point is significant to the magnetic resonance imaging (MRI) magnets. This new flux pump is under construction presently. It is expected that the Bi2223 flux pump would be applied to the superconducting MRI magnets by further optimizing structure and improving working process.     

环境土壤样品中~(99)Tc的分析方法研究进展

随着核能的开发及核医学诊断的发展,~(99)Tc的研究日益受到重视。~(99)Tc具有半衰期长、裂变产额高和迁移性强等特点,在核废物的地质处置、环境安全评价及生物效应方面倍受关注,准确测定环境土壤样品中~(99)Tc的含量显得至关重要。本文在文献调研的基础上较详细总结了Tc的化学性质,并对~(99)Tc分析流程中样品的预处理、化学分离纯化、制源及测量等过程中涉及的主要方法进行了综述,指出了现今分析方法中存在的主要瓶颈,并对环境样品中~(99)Tc的分析做了展望。     

~(99)Tc~mN-DMSA的制备及其生物分布

以SnCl2 ·2H2 O为还原剂 ,丁二酰二酰肼 (SDH)为N3 -离子提供体 ,在室温下制备 [99TcmN]2 + 中间体 ,然后与二巯丁二酸 (DMSA)发生配体交换反应 ,得到放射化学纯度大于 90 %的 99TcmN DMSA配合物。99TcmN DMSA在室温下 6h内稳定 ,脂水分配系数lgP =- 3.74 ,表明是一水溶性化合物。99TcmN DMSA在小鼠体内生物分布表明 ,与作为肾显像剂的99Tcm DMSA相比 ,其生物分布发生了较大的变化 ,99TcmN核的引入导致了较高的骨摄取值和较低的肾摄取值     

~(99)Mo-~(99m)Tc平衡源中~(99m)Tc和~(99)Mo强度比测定

本文用4πβ-γ符合方法中的外推吸收法测定了~(99)Mo-~(99m)Tc平衡源中的总“β”强度,用准确标定过的~(99m)Tc标准源刻度好效率的S-80多道高纯锗γ谱仪测定平衡源中~(99m)Tc的绝对强度,从而测定了~(99m)Tc和~(99)Mo的强度比。结果为0.974±0.0023。并将结果和编评值比较,为~(99)Mo的绝对标定提供了~(99m)Tc的修正量为0.1088±0.0023的实测值。     

Comparative Preclinical Evaluation of Peptide-Based Chelators for the Labeling of DARPin G3 with 99mTc for Radionuclide Imaging of HER2 Expression in Cancer

Non-invasive radionuclide imaging of human epidermal growth factor receptor type 2 (HER2) expression in breast, gastroesophageal, and ovarian cancers may stratify patients for treatment using HER2-targeted therapeutics. Designed ankyrin repeat proteins (DARPins) are a promising type of targeting probe for radionuclide imaging. In clinical studies, the DARPin [^99mTc]Tc-(HE)₃-G3 labeled using a peptide-based chelator His-Glu-His-Glu-His-Glu ((HE)₃), provided clear imaging of HER2 expressing breast cancer 2–4 h after injection. The goal of this study was to evaluate if the use of cysteine-containing peptide-based chelators Glu-Glu-Glu-Cys (E₃C), Gly-Gly-Gly-Cys (G₃C), and Gly-Gly-Gly-Ser-Cys connected via a (Gly-Gly-Gly-Ser)₃-linker (designated as G3-(G₃S)₃C) would further improve the contrast of imaging using ^99mTc-labeled derivatives of G3. The labeling of the new variants of G3 provided a radiochemical yield of over 95%. Labeled G3 variants bound specifically to human HER2-expressing cancer cell lines with affinities in the range of 1.9–5 nM. Biodistribution of [^99mTc]Tc-G3-G₃C, [^99mTc]Tc-G3-(G₃S)₃C, and [^99mTc]Tc-G3-E₃C in mice was compared with the biodistribution of [^99mTc]Tc-(HE)₃-G3. It was found that the novel variants provide specific accumulation in HER2-expressing human xenografts and enable discrimination between tumors with high and low HER2 expression. However, [^99mTc]Tc-(HE)₃-G3 provided better contrast between tumors and the most frequent metastatic sites of HER2-expressing cancers and is therefore more suitable for clinical applications.     

~（99m）Tc（V）－DMSA大鼠体内药代动力学

用改良方法成功制备了五价锝标记的二巯基丁二酸（９９ｍＴｃ（Ｖ）－ＤＭＳＡ）。根据血样时间－放射性曲线，该药在大鼠体内的代谢符合开放型二房室模型。主要动力学参数为Ｔ１／２（α）＝３．４ｍｉｎ，Ｔ１／２（β）＝７０．９ｍｉｎ，Ｖ（ｃ）＝２７２ｍｌ，Ｋ２１＝０．０５８ｍｉｌ－１，Ｋ１０＝０．０３４ｍｉｎ－１，Ｋ１２＝０．１２２ｍｉｎ－１。结果表明，９９ｍＴＣ（Ｖ）－ＤＭＳＡ从血液向组织的分布速度快，分布范围极广，体内消除迅速，基本从血中清除仅需６—７ｈ．为该显像剂的临床应用提供了实验基础。还研究了该药在大鼠血中的存在形式。     

一种肾脏显像剂的研制

报道自行合成氯化Ｎ－甲基吡哆醛（ＳＢ），研究了甘氨酸（Ｇｌｙ），丙氨酸（Ａｌａ），甘氨酸乙酯（ＧｌｙＯＥｔ）与ＳＢ形成的碱，在ＳｎＣｌ２．２Ｈ２Ｏ存在下，与锝螯合后体内的代谢，还研究了影响标记率的因素和标记的最佳方法，用＾９９ｍＴｃ－Ｓｂ－Ｇｌｙ作动物实验的研究结果表明，这种阳离子螯合剂静脉注射后均能快速地经肾脏排出体外，３０ｍｉｎ尿排泄率为７９．６８±６．６６ＩＤ％，略低于＾９９Ｔｃ－ＤＴＰＡ（