~(99)Tc~m标记多巴胺D_2受体配体的合成,标记及生物分布研究

首次合成了3种苯酰胺类D2受体配体：N-[（2-巯基）乙基]-2，3-二甲氧基苯甲酰胺（MEDM-BZM），N-[（2-巯基）乙基]-5-溴-2，3-二甲基苯甲酰胺（MEBDM-BZM），N-[（2-巯基）乙基]-3-乙氧基苯甲酰胺（MEE-BZM），光谱数据与结构相符。用配体交换法与3-硫杂-1，5-戊二硫醇共同配位合成了中性脂溶性“3 1”型混配^99Tc^m螯合物，标记率在于85%。3种配合物在小鼠脑中的初始摄取率高于文献报道值。     

~(99)Tc~m标记的N-(邻甲硫基苯基)乙二胺和硫醇混配配合物的制备及生物分布

合成了新的三齿配体N-(邻甲硫基苯基)乙二胺(MTPEA)，并经IR、元素分析、MS(FAB^ )表征确认。确定了混配配合物^99Tc^m(L3,L1s)(L3为MTPEA，L1s为乙硫醇)和^99Tc^m(L3，L1b)(L1b为异丙硫醇)的最佳标记条件。标记物在小鼠体内的生物分布结果表明：这两种配合物都可以通过正常的血脑屏障，并在脑中有一定的滞留。在注射后2，30min，^99Tc^m(L3，L1s)的脑摄取值分别为2．09％／g和1．10％／g；^99Tc^m(L3，L1b)的脑摄取值分别为1．76％／g和l.08％／g。     

99Tcm-MAG2-Ade肿瘤显像剂的合成及其生物活性研究

为了制备肿瘤显像剂^99Tc^m标记肽,合成并表征了新的碱基修饰的小肽配体9-[N-(S-三苯甲基巯基乙酰)二甘氨酰氨基乙基]腺嘌呤(Tr—MAG2-Ade)。通过直接标记法得到了水溶性配合物^99Tc^m-MAGz—Ade,并对其体外稳定性进行了检测。在荷瘤小鼠体内的生物分布结果表明,^99Tc^m-MAGz—Ade在肿瘤中有较高的摄取,肿瘤与肌肉的摄取比为5．7,肿瘤与血液的摄取比为1．55。血液清除较快,有望用于非腹部肿瘤的显像。     

5 ^99Tc^m（CO）3-IDA-FAC11的制备及生物分布

放射性核素标记脂肪酸作为心肌代谢显像剂可进行局部缺血定位及评价梗塞区心肌的活力。在SPECT显像药物中，锝[^99Tc^m]药物占有主导地位，因此，^99Tc^m标记的心肌脂肪酸代谢显像剂将有非常好的应用前景。本实验对象为二（N-乙酸）-十一烷酸（HOOC（CH2）10N（CH2COOH）2，IDA—FAC11），以[^99Tc^m（CO）3（H2O）3]^＋为中间体，合成了^99Tc^m（CO）3-IDA—FAC11，建立了^99Tc^m（CO）3-IDA—FAC1l放化纯的高效液相色谱法（HPLC）分析方法。研究了反应时间、温度、pH值和配体用量等对标记物产率的影响。     

^99Tc^m标记5—HT1A脑受体显像剂的研制及其生物分布

为了寻找99Tcm标记中枢神经系统5-HT1A协同受体显像药物,合成了单齿受体配基1-(2-甲氧基苯基)-4-(2-巯基乙基)哌嗪(简称MPMEP)、三齿配体N,N-二(2-巯基乙基)-N',N'-二乙基乙二胺(简称BMPDEEDA)和N,N-二(2-巯基乙基)卞胺(简称BMPBA),其结构经IR、NMR及元素分析表征;以“3+1”混合配体进行了99Tcm标记,并确定了标记反应的最佳条件pH=6.0～7.0,60～70℃下,反应20～30min,经CH2Cl2萃取脂溶性部分后,99TcmO(MPMEP)(BMPDEEDA)和99TcmO(MPMEP)(BMPBA)的标记率分别达到95%和90%以上.采用HPLC对标记产物进行了分离和纯化,纯化后的标记物放化纯度均>98%.小鼠体内的生物分布结果表明99TcmO(MPMEP)(BMPDEEDA)和99TcmO(MPMEP)(BMPBA)配合物可以通过血脑屏障,在脑中有一定的摄取和滞留;99TcmO(MPMEP)(BMPBA)在血液中清除较快,静脉注射后2、30、60min时,脑与血摄取比分别为0.31、0.33、0.32,但血液中放射性活度仍然较高.     

99TCm-MDP、99TCm(V)-DMSA和99Tcm-Citrate显像对骨组织良恶性疾病鉴别诊断的对比研究

为评价^99Tc^m(V)-二巯基丁二酸钠(DMSA)显像和^99Tc^m-枸缘酸(Citrate)显像在骨转移癌和骨及骨关节炎症诊断中的意义，对骨转移癌患者和骨及骨关节炎症患者各18例分别进行^99Tc^m-亚甲基二膦酸(MDP)、^99Tc^m(V)-DMSA和^99Tc^m—Citrate全身显像，并比较了它们的显像结果。18例经病理学、CT或MRI证实有骨转移癌的患者，^99Tc^m-MDP显像共检出64个病灶，^99Tc^m(V)-DMSA显像显示在与^99Tc^m-MDP显像相同部位同检出49个病灶，而^99Tc^m—Citrate显像仅检出1个病灶。18例经细菌学、cT或MRI证实的骨及骨关节炎症患者，^99Tc^m—MDP显像共检出22个病灶，^99Tc^m(V)-DMSA显像显示在与^99Tc^m-MDP显像相同部位同检出l7个病灶，^99Tc^m-Citrate显像检出l6个病灶。本组病例^99Tc^m(V)-DMSA显像诊断骨转移癌的灵敏度为76．56％，特异性为22．73％；^99Tc^m-Citrate显像诊断骨转移癌的灵敏度仅为1．56％，特异性为27．27％,^99Tc^m(V)-DMSA显像诊断骨及骨关节炎症的灵敏度为77．27％，特异性为23．44％；^99Tc^m-Citrate显像诊断骨及骨关节炎症的灵敏度为72．73％，特异性为98．44％。以上结果表明，^99Tc^m（V）-DMSA显像在诊断骨转移癌和骨组织炎症时应该慎重，因为它不能区分骨组织的良恶性病变性质，其对骨组织的良恶性病变性质的鉴别诊断应排除外骨组织炎症、骨折等骨组织良性病变的干扰。而^99Tc^m—Citrate显像对于骨及骨关节炎症诊断特异性比^99Tc^m-MDP骨显像和^99Tc^m（V）-DMSA骨显像都高。     

99TcmN-DMCHI和99Tcm-DMCHI的制备及其生物分布

合成并表征了新的异腈配体2,3-二甲基环己基异腈(DMCHI)及其铜络盐。分别通过配体交换法和直接标记法制备得到放化纯大于95％的脂溶性配合物^99Tc^mN-DMCHI和^99Tc^m-DMCHI,二者在室温下均可稳定6h以上。在正常小鼠体内的生物分布实验结果表明,^99Tc^mN-DMCHI和^99Tc^m-DMCHI在血液中均有较高的摄取和很好的滞留,而且血／心、血／肝和血／肺比值均大于1,有望用于心血池显像。     

一种99Tcm标记的5-HT1A受体显像剂的合成与标记

合成了一种^99Tc^m标记的5-HT1A受体显像剂。该显像剂先由二硫二氮与6-溴己酰氯结合，再与2-（1-哌嗪）苯甲醚结合，经还原、脱保护反应得到标记前体，再对前体进行^99Tc^m标记。标记率达90％以上，薄层层析测得标记物放化纯度大于95％。     

[99Tcm(CO)3(H2O)3]+标记的新双功能联接剂的研究

设计合成了3种新的小分子三齿配体NNS-1,NNS-2,NSN,并设计合成了文献报道的NNO三齿配体。它们作为双功能联接剂可以连接受体、多肽、蛋白等靶向性分子,用于设计合成新的以[^99Tc^m(CO)3]为核心的放射性药物。标记条件实验证明,3种新配体在配体量极低(10μg)、在较短的反应时间内(10min),配体标记率可以达到95％以上,放射化学纯度大于90％,均为高效的双功能联接剂;电泳实验和脂溶性实验表明：NNS-1,NNS-2,NSN与羰基锝标记后,锝配合物显示不同价态;稳定性实验证明,3种标记物均具有很高的体外稳定性,标记后6h内基本不分解;GSH,L-半胱氨酸体外竞争稳定性实验证明其不易受到裸露-SH的进攻,因而在体内也会有较高的稳定性;小鼠动物分布试验表明,3个配合物均能较快地从血液和多数组织器官中清除,主要在肝脏浓集,是较理想的标记[^99Tc^m(CO)3(H2O)3]^ 的双功能联接剂。     

99Tcm-EC-ASODN反义探针的合成和标记

报道反义探针^99Tc^m-EC-ASODN的合成和标记。将次乙酰双半胱氨酸(L，L-ethylene dicysteme,EC)与反义寡脱氧核苷酸(Antisense oligodeoxynucleotides，ASODN)进行偶联，形成复合物EC-ASODN，通过核磁共振图谱(^1H—NMR)、红外图谱(IR)、紫外(A260)吸收和电泳，鉴定EC-ASODN复合物的结构。用锝(^99Tc^m)标记EC-ASODN，通过薄层层析评价^99Tc^m．EC-ASODN的标记率、放化纯和稳定性。结果显示，^1H-NMR、IR谱图、紫外吸收和电泳都证实EC与ASODN联结形成EC-ASODN，^99Tc^m-EC-ASODN的标记率为77．28％，放化纯为97．52％，Rr=0．95—1，4h内具有很好的稳定性。结论：EC与ASODN能形成稳定的复合物EC-ASODN，用^99Tc^m标记，方法简便，能得到标记率高和稳定性好的反义探针。     

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.     

有效探测面积大于1000 cm2的正比计数器测量系统性能测试

为对自制的活性面积高达1 000 cm²的大面积源进行表面发射率定值,同时作为现有2πα、2πβ表面发射率标准装置能力的扩充,研制了一套内置式大面积2π多丝正比计数器测量系统,并利用活性区直径为8 mm的²⁴¹Am点源及活性区面积为10 cm×15 cm的大面积²⁴¹Am和⁹⁰Sr-⁹⁰Y源对其进行计量学性能测试。结果表明：计数器内计数响应均匀性优于±0.4%,有效探测面积达1 400 cm²;所得²⁴¹Am源高压坪曲线的坪长为1 400 V,坪斜为0.27%/100 V,坪区内计数变化为0.87%;⁹⁰Sr-⁹⁰Y源高压坪曲线的坪长为300 V,坪斜为0.75%/100 V,坪区内计数变化为0.80%;10次测量重复性好于0.4%,8 h内短期稳定性好于0.3%,1 a内长期稳定性好于0.8%。     

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.