多巴胺D2受体显像剂99Tcm-MBZM的合成及生物性能评价

本工作以舒必利(Sulpiride)为分子模型,在芳环的5位上引入巯基(替代磺酰胺基)合成了(S)-(-)-5-巯基-N-[(1-乙基-2-吡咯烷基)甲基]-2-甲氧基苯甲酰胺 [简写为MBZM ]左旋异构体.通过"3+1"(二元混合配体络合)方案,合成了一种新的D2受体显像剂99Tcm-MBZM.其在大鼠体内的生物分布实验结果显示,99Tcm-MBZM在血液中的清除较快,30 min后降到0.444 %ID/g;在肝和肾脏中的放射性则持续较高,30 min后仍分别达2.148和2.184 %ID/g;在脑中的摄取量偏低,2 min 时仅为0.145 %ID/g.因此99Tcm-MBZM不能作为脑受体显像剂.     

~(99)Tc~mN-CHDTC的制备,生物分布及与~(99)Tc~m-CHDTC的对比

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 +int 中间体 ,然后与二水·N 环己基 二硫代氨基甲酸钠 (CHDTC)发生配位体交换反应得到放化纯大于 90 %的99TcmN CHDTC配合物。小鼠体内的生物分布实验表明 ,99TcmN CHDTC有较高的脑摄取和较好的脑滞留。注射后 5,30 ,6 0min时 ,脑摄取量 (% /g)分别为 2 91,5 88,5 91,R(脑 /血 )比值分别为 0 14,1 4 6 ,2 10。99TcmN CHDTC在心肌中也有较高的摄取 ,但R(心 /肝 )比值低。采用甲脒亚磺酸 (FSA)作还原剂对配位体CHDTC进行99Tcm 直接标记 ,其在小鼠体内的生物分布结果表明 ,99Tcm CHDTC主要蓄积在肝脏 ,脑、心肌摄取很少。这表明放射性药物分子中引入 [99TcmN]2 +核会引起生物分布性质的明显改变     

~(99m)TcN-IBDTC与~(99m)Tc-IBDTC的对比研究

为了检验配合物分子中 [99mTcN]2 + 中心核的引入对其生物分布的影响以求找到一种新的放射性药物。采用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[99mTcN]2 + int 中间体 ,然后与配体N -异丁基 -二硫代氨基甲酸钠 (IBDTC)发生配体交换反应得到99mTcN -IBDTC配合物。同时采用甲脒亚磺酸 (FSA)作还原剂对配体IBDTC进行了99mTc直接标记。结果表明 ,99mTcN -IBDTC和99mTc -IBDTC配合物的放化纯均大于 90 % ,小鼠体内生物分布表明 ,99mTcN -IBDTC有较高的脑摄取和较好的脑滞留 ,在注射后 5、30、6 0min时脑摄取量 (%ID·g- 1)分别为 6 .2 2、5 .4 5、3.88,脑 /血比值分别为 1.5 1、2 .2 4、1.84 ,有望成为一类新型脑灌注显像剂。99mTcN -IBDTC在心肌中也有较高的摄取 ,但心肌清除快而且心 /肝比值低从而限制了其成为一类新型心肌灌注显像剂。99mTc -IBDTC主要在肝内浓集 ,而脑、心肌摄取很少。本实验提示 ,放射性药物分子中引入 [99mTcN]2 + 核会引起生物分布性质的明显改变 ,这对于设计新型放射性药物具有参考价值。     

肝受体显像剂99Tcm-HYNIC-NGA的制备与初步评价

在NGA分子上引入双功能连接剂HYNIC制备了HYNIC-NGA,选用HEDTA及Bicine两种共配体对其进行了99Tcm的标记,考察了标记物在正常小鼠体内的生物分布,并用GSA作为抑制剂(注射剂量10 mg/kg)对99Tcm-HEDTA/HYNIC-NGA进行了抑制实验.结果显示,99Tcm-bicine/HYN...     

~(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)Tc~mN-CHDTC的制备,生物分布及与~(99)Tc~m-CHDTC的对比

以SnSl2.2H2O为还原剂，丁二酰二酰肼（CDH）为N^3-离子提供体，在室温下制备[^99Tc^mN]int^2 中间体，然后与二水.N－环己基－二硫代氨基甲酸钠（CHDTC）发生配位体交换反应得到放化纯大于90％的^99Tc^mN-CHDTC合物化。小鼠体内的生物分布实验表明，^99Tc^mN-CHDTC有较高的脑摄取衅好的脑滞留。注射后5，30，69min时，脑摄取量（％／g)分别为2．91，5．88，5．91，R（脑／血）比值分别为0．14，1．46，2．10。^99Tc^mN-CHDTC在心肌中也有较高的摄取，但R（心／肝）比值低。采用甲脒亚磺酸（FSA）作还原剂对配位体CHDTC进行^99Tc^m直接标记，其在小鼠体内的生物分布结果表明，^99Tc^m-CHDTC主要蓄积在肝脏、脑、心肌摄取很少。这表明放射性药物分子中引入[^99Tc^mN]^2 核会引起生物分布性质的明显改变。     

受体显像剂~(99m)Tc-NCAM在小鼠脑组织中的药物代谢动力学研究

对N-甲基-D-天冬氨酸(NMDA)受体拮抗剂锝标记N-[2-(N-(2-巯基乙基))氨基乙酰基]-N-(2-巯基乙基)-3,5-二甲基金刚烷胺基乙酰胺(99mTc-NCAM)进行小鼠脑组织中药物动力学研究。KM小鼠尾静脉注射0.2mL(7.4MBq)99mTc-NCAM,分别于注射后5、10、30、60、120、180min处死,取大脑皮层、纹状体、海马、小脑和丘脑,称重和测计数。以相同的时间点,小鼠断尾取血20μL,测计数。用药物动力学定域模型进行脑组织和血药动力学研究。结果表明,99mTc-NCAM静脉注射给药后迅速进脑,在大脑皮层和海马有较高的摄取,最高摄取分别为1.51±0.13%ID/g和0.74±0.002%ID/g。理论计算表明,99mTc-NCAM在小鼠体内符合二室模型,并获得各种脑组织和血液的药物动力学方程和参数。99mTc-NCAM能透过血脑屏障进入小鼠脑内特定区域,以NMDA受体分布最多的大脑皮层和海马摄取较多,可望成为一种新的NMDA受体显像剂,用于一些神经退行性疾病的诊断预后等。     

~(99m)Tc-帕米膦酸盐的制备及骨分布

为观察99mTc标记的帕米膦酸盐(Pamidronate,PAM)的骨分布特点,以氯化亚锡为还原剂,优化99mTc直接标记PAM的条件,研究SnCl2(Ⅱ)含量、配体用量、pH及反应时间对标记率的影响,确定了优化的标记条件;考察99mTc-PAM的体外稳定性;评价99mTc-PAM在正常鼠体内的生物分布,尤其是骨摄取情况,比较99mTc-PAM与99mTc-MDP在正常小鼠体内的骨摄取。实验结果表明,PAM的99mTc标记方法简单,标记率大于95%,标记物体外稳定性好。正常鼠体内分布实验发现,99mTc-PAM骨摄取很高,且滞留时间长,在血液中清除快,在体内主要通过肾代谢;正常大鼠SPECT显像骨组织清晰可见,具有很好骨显像效果。与99mTc-MDP在正常小鼠体内的生物分布结果比较表明,99mTc-PAM的骨放射性摄取及骨与血放射性摄取比在不同时相均优于99mTc-MDP。研究表明,99mTc-PAM具有理想的骨显像性能,可用于骨显像、骨损伤探测以及肿瘤骨转移检测等应用研究。     

[99TcmN(PNP)]2+标记葡萄糖硫酮类衍生物混配配合物的研究

为研究新的99TcmN核心标记的心肌和肿瘤显像药物,选用自行合成的二硫化碳-葡萄糖(硫酮类)衍生物Ln(L1～L5)制备一系列带有葡萄糖衍生物基团的新型[99Tcm (DTC)(PNP)]+类配合物,经TLC和HPLC检测,配合物的放射化学纯度均大于90%.小鼠生物分布实验表明,99TcmN(PNP)Ln(L1～L5)系列配合物在正常小鼠体内初始的放射性摄取主要分布于心肌、肝、肺、肾等脏器,并且30 min内各脏器均可迅速清除.初步的荷EMT-6鼠生物分布实验显示,99TcmN(PNP)L2在肿瘤中放射性摄取不高,30 min时为(0.39±0.03)%ID/g,其它组织的放射性摄取与正常小鼠类似.     

Aβ显像剂SUP>99/SUP>TcSUP>m

制备了新的Aβ斑块显像剂99Tcm-酰胺基氨基二硫醇(MAMA)-4-氨基-4′-二甲氨基联苯(DMABP),并研究了其在正常小鼠体内的生物分布。实验结果表明,99Tcm-MAMA-DMABP具有较高的初始脑摄取,较快的正常脑组织清除,尾静脉注射后2 min的脑摄取达0.88%/g,2 min与60 min的脑摄取率比值为2.8。     

Preparation of Zn/TiO2 powder and its photocatalytic performance for oxidation of P-nitrophenol

Zn-doped TiO2 catalysts were prepared using a sol-gel method and characterized by XPS,UV-Vis, BET, XRD in this study. Under the irradiation of simulant sunlight, the photocatalytic activity for the degradation of p-nitrophenol was studied too. After irradiation for 2.5 h, the degradation percentage of p-nitrophenol could rise to more than 80 %. The results showed that the spectrum absorption band edge of Zn/TiO2 powder does not broaden obviously comparing with pure TiO2 powder. Zinc exists as Zn （11）. When calcined at 973 K, there is a new phase as ZnTiO3 in Zn/TiO2 catalyst. The order of photocatalytic activity of Zn/TiO2 catalysts calcined at different temperatures for p-nitrophenol is 773 K 〉 673 K 〉 873 K 〉 573 K 〉 973 K and the photocatalytic activity of Zn/TiO2 catalyst calcined at 773 K is better than TiO2 catalysts heated at the same temperature, and outclasses that of commercial TiO2 catalyst. It also showed that the photocatalytic degradation of p-nitrophenol follows first-order kinetics under the irradiation of simulant sunlight.     

Current status of radiation therapy for prostate cancer

Radiotherapy for the treatment of prostate cancer has been extensively explored in the past. Along with the comprehensive understanding of the biology of prostate cancer and rapid advances in terms of technology, the out- come of treatment for the patients with prostate cancer has improved. The authors review radiotherapy as the primary treatment for the disease, with particular emphasis on the technological advances from both the radiobiological and radiophysics aspects. Nonconventional fractionated irradiation like hyper- or hypo-fractionation has been imple- mented in the clinic, the final results still need to be confirmed in the future. Technological advances like IMRT, IGRT, in the last two decades have significantly improved the delivery of external radiotherapy to the prostate. This has re- sulted in an overall increase in the total dose that can be safely delivered to the prostate, which has led to modest im- provements in the biochemical outcome. However, establishing the standard therapy for prostate cancer remains con- troversial. It is hoped that the next decades will bring continued advances in the development of biologicals that will further improve current clinical outcomes.     

The control system for SSRF injection and extraction

This paper introduces the injection and extraction control system design for SSRF,which is a distributed control system aimed at stability and reliability of the pulse power supplies,PPS(Personnel Protection System)and MPS(Machine Protection System).The hardware environment is mainly based on PLC(Programmable Logic Con- troller),and ARM(Advanced RISC Machine)is also applied for studying stability of the power supplies.WinCC and EPICS(Experimental Physics and Industrial Control System)have been selected as the platforms of SCADA(Super- visory Control and Data Acquisition).For unifying the interfacing to the control computer,all front-end equipments are connected via Industrial Ethemet.     

水平管内含空气蒸汽强制对流冷凝换热模型研究

为研究含空气蒸汽在水平管内强制对流冷凝换热特性,基于对传热传质过程的分析,建立了管内为环状流与波状流条件下的流动冷凝换热模型。从潜热、显热和液膜3个环节对整个换热过程进行建模,最终得到计算局部冷凝换热系数的理论关系式。模型预测结果与实验数据的对比表明,二者相对偏差在±20%以内,验证了该换热模型的准确性与适用性。通过进一步的研究发现：从换热管入口至出口,随着冷凝的进行,管内换热主要热阻由液膜热阻向气液界面的凝结热阻转变;主流气体对流换热过程基本可忽略。     

Investigations on landmine detection by BF3 detector

Experiments were carried out to investigate the possible use of neutron backscattering for the detection of polyethylene (PE) sample buried in the soil. In detection of landmine by neutrons, the neutron detector and its shield play an important role. In this paper, the effects of graphite, heavy water, polyethylene and boric acid moderators on the flux of back scattered neutrons were investigated. We have also experimentally verified the effect of BF3 detector shield and obtained good agreement with theory.     

Web Services interface of SSRF archive data analysis system

Accelerator database stores various static parameters and real-time data of accelerator. SSRF (Shanghai Synchrotron Radiation Facility) adopts relational database to save the data. We developed a data retrieval system based on XML Web Services for accessing the archive data. It includes a bottom layer interface and an interface applicable for accelerator physics. Client samples exemplifying how to consume the interface are given. The users can browse, retrieve and plot data by the client samples. Also, we give a method to test its stability. The test result and performance are described.     

Assessment of radioactivity levels in some oil samples from the western desert, Egypt

Distributions of natural gamma-emitting radionuclides were determined in 93 oil samples collected from some petroleum fields in the western desert of Egypt. The radioisotope activities in the area under investigation lay in the range of (21 ± 4) to (38 ± 13) Bq?L-1 for 226Ra, (9 ± 2) to (15 ± 5) Bq?L-1 for 232Th, and (154 ± 28) to (303 ± 54) Bq?L-1 for 40K. The mean values were 27, 12, and 201 Bq?L-1, respectively. Among oils, variations in radionuclide ac- tivities could be on account of differences in TDS, HCO3, and Ba, with high or low pH. In this environment, oil prop- erties differently affected the mobilization of natural radionuclides. The range of 226Ra variation had been compared with available data from other countries. The calculated absorbed dose rate ranged from 22.33 to 32.66 nGy?h-1 in lo- cation (B) and (E) respectively, which was less than the accepted value.     

Preparation and properties of 117m Sn(IV)-TTHMP in in-vitro and in small animals

In this work,TTHMP was synthesized and labelled with 117m Sn.The preparation conditions,stability and lipophilicity of 117m Sn(IV)-TTHMP were investigated.Biodistribution of the complex in rabbits and mice was studied.It was found that the quantity of TTHMP and pH value of the prepararion solution had vital effects on the labeling yield of 117m Sn(IV)-TTHMP.It was also found that 117m Sn(IV)-TTHMP was hydrophilic and stable at room temperature and 37℃ in open air 117m Sn(IV)-TTHMP showed unexpectedly high bone uptake and bone-to-blood ratio in the animals.This made it potentially useful as an reagent for skeletal scintigraphy and radiotherapy of bone tumors.     

The role of AGFA high-energy CR in the calibration and quality control of multileaf collimators （MLC）

Linear accelerators equipped with multileaf collimators （MLC） are becoming more common and are widely used in the intensity-modulated radiotherapy （IMRT）. There is an imperative need to ensure the commissioning specification of the linear accelerators for the sake of quality assurance （QA） and quality control （QC）. This paper is aimed to investigate the role of AGFA high-energy CR （Computed Radiography） in calibrating dynamic multileaf collimators and evaluating the accuracy of the leaf position. The result shows that AGFA high-energy CR can easily and conveniently be used to calibrate MLC and verify its position. Hence, the application of AGFA high-energy CR is proved to be an accurate and time-saving method for routine MLC QC, especially when MLC calibration adjustments are required.     

Gamma radiation levels in the ambient environment of the QNPP Base

Monitoring results of gamma dose rate level in 1992～2004 in the ambient environment of the Qinshan Nuclear Power Plants(QNPP)Base,the northeast of Zhejiang Province,are reported in this paper.It is shown that the gamma dose rate of five monitoring sites of 2.5 km to QNPP Base is 84～113 nGy/h,with an average of 96 nGy/h in the 13 years.The average value is close to the background level of 93 nGy/h prior to operation of the QNPP Base,and is lower than the monitoring result of 101 nGy/h at the reference site in Hangzhou City.Within 50 km from the QNPP Base,the cumulative dose rate of the thermoluminescent dosimeter(TLD)is 90 nGy/h,which is lower than the back- ground level of 111 nGy/h.