^123I—β—CIT：一种新型多巴胺转运体显像剂

^123I-β-CIT是一种新型多巴胺转运体SPECT显像剂,具有亲和力高,脑滞留时间长,以及纹状体与小脑摄取比较高等特点。它对帕金森氏病的早期诊断、临床分期、疗效观察有较高的临床应用价值。本文介绍了^123I-β-CIT在标记、药物动力学、毒性及临床应用等方面的研究结果,并提出了今后在DAT显像剂方面的发展方向。     

125I-β-CIT动物体内生物学分布研究

了解多巴胺转运体显像剂＾１２５Ｉ－β－ＣＩＴ在体内的生物学分布情况,为其临床应用提供客观依据。采用Ｉｏｄｏｇｅｎ标记法制备＾１２５Ｉ－β－ＣＩＴ,用ＨＰＬＣ进行分离纯化与鉴定,体内生物学分布用ＮＩＨ小鼠,脑放射性自显影用ＳＤ大鼠。结果表明：＾１２５Ｉ－β－ＣＩＴ标记率为８４％,放比纯度大于９８％;ＮＩＨ小鼠血液清除,１２ｈ内符合二室模型（α＝３．８７,β＝０．１６２,Ｔ１／２α＝０．１７９,Ｔ１／     

~(125)I标记多巴胺D_3受体显像剂的合成

制备了12 5I标记的具有多巴胺D3 受体潜在活性的核药物12 5I 7 OH PIPAT(7 羟基 2 (N 丙基 N 3’ 碘 2’ 烯丙基 )氨基四氢萘满 )。从化合物 2 ,7 二羟基萘开始 ,经过多步反应合成出12 5I 7 OH PIPAT的前体 ,并对它进行12 5I标记。12 5I 7 OH PIPAT经分离纯化后 ,检测结果为 :放射化学产额为 5 7% ,放化纯度大于86 %。     

BMIPP的合成与125I标记

报道了由ω－溴十一烷酸制备β－甲基－对磺苯代十五烷酸的合成方法。 物经红外,核磁共振,元素分析和质谱等方法确证。同时报道了ＢＭＩＰＰ的＾１２５Ｉ标记方法,经ＴＬＣ检测,标记率和放化纯度分别大于８０％和９８％。     

多巴胺D2受体显像剂^125I—IBZM的合成与标记

合成了标记前体Ｓ－（－）－２－羟基－６－甲氧基－Ｎ－［（１－乙基－２－吡咯烷基）甲基］苯甲酰胺（Ｓ－（－）－ＢＺＭ）。光谱数据与结构相符。以Ｓ－（－）－ＢＺＭ为前体，用１２５Ｉ－ＮａＩ标记，成功地制备了Ｓ－（－）－３－１２５Ｉ－２－羟基－６－甲氧基－Ｎ－［（１－乙基－２－吡咯烷基）甲基］苯甲酰胺（Ｓ－１２５Ｉ－ＩＢＺＭ）。标记率大于８０％，放射化学纯度大于９０％，整个制备过程仅需４５ｍｉｎ，利于药盒化生产。     

~(125)I标记多巴胺D_3受体显像剂的合成

制备了^125I标记的具有多巴胺D3受体潜在的活性的核药物^125I-7-OH-PIPAT(7-羟基-2（N-丙基-N-3'-碘-烯丙基）氨基四氢萘满)。从化合物2，7-二羟基萘开始，经过多步反应合成出^125I-7-OH-PIPAT的前体，并对它进行^125I标记。^125I-7-OH-PIPAT经分离纯化后，检测结果为：放射化学产额为57%，放化纯度大于86%。     

偶联心得宁衍生物的合成,^125I标记和动物实验

对偶联心得宁衍生物的合成，＾１２５Ｉ标记和动物体内分布实验进行了研究。结果表明，由于该药物具有双配位基因，对β受体的亲和力比单价配基要高５０多倍，给药后大鼠心血比持续升高，在４ｈ达到峰值，因此该药物有可能成为心肌受体显像剂。     

多巴胺D2受体显像剂Epidepride的合成及其^131I标记

以3－甲氧基水杨酸为原料合成了Epidepride[S-(-)-N-[1-乙基－2－吡咯烷基]-5－碘－2,3－二甲氧基基甲酰胺]及其标记前体（S－（－）－5－（三正丁基锡）－N（1－乙基－2－吡咯烷基）甲基]2,3-二甲氧基苯甲酸酰胺）,并采用双氧水法对标记前体进行^131I标记,获得了^131I-epidepride,标记率和放化纯度均大于95％。132I-epidepride溶液体外稳定性好,4℃放置15d放化纯度仍大于90％。^131I-epidepride与D2受体亲和力高,大鼠脑内纹状体与小脑的摄取比在320min时高达237;在脑内纹状体的吸收可被Spiperone安全阻断。因此,^131I－epideride有望成为多巴胺D2受体SPECT显像剂。     

多巴胺转运蛋白显像剂^18F—FP—β—CIT的制备

可卡因经水解、脱水、甲酯化、苯基溴镁格氏反应、脱N－甲基、碘化、N烷基化、甲磺酰化等反应制备氟标记前体,用K222催化进行氟标记,得到^18F-FP-β-CIT[N－（3－氟丙基）－2β－甲酯基－3β－（4‘－碘苯）去甲基托烷],标记率25％－30％,放射化学产率10％－12％,合成及纯化时间100－110min,纯化后放化纯度＜95％,稳定性较好。     

6—[^18F]氟—L—多巴的合成与制备技术进展

介绍了合成6－[^18F]氟－L－多巴的意义和制约因素，亲电取代法和亲核取代法的主要原理、考虑因素和一些具有代表性的合成路线，并对这两类方法进行了比较。     

Increase in internal friction in uranium with change in temperature

On the basis of the previously described increase in internal friction in uranium during heating, a semiquantitative evaluation was made of the dependence of increase in internal friction on the rate of heating, frequency and amplitude of vibrations. The results of the calculations agree satisfactorily with data obtained experimentally. A study was made of the effect of the initial state of the specimen on the increase in internal friction at the initial stages of heating.     

广东省进出口食品中的放射性检验

报道了广东省商检中心放射性检验室开展的广东进出口食品中的放射性检验工作。介绍了检验工作采用仪器的主要性能及应用;给出了分析测量方法和探测下限以及实验的质量保证措施,并给出了检验室测量的广东省几种食品中的放射性含量范围,测量结果与我国食品中放射性活度变化范围大体一致。     

Tritium concentrations in precipitation in Shanghai

Tritium concentrations in precipitation can be used as a criterion to evaluate the tritium baseline of the environment. The tritium concentration in precipitation in Shanghai during 2014-2015 was determined. Values ranged from 0.68 ± 0.04 to 4.11 ± 0.39 Bq/L, and it showed a decreasing trend compared with historical data; however,the values were slightly higher than the natural background tritium level. Additionally, the tritium concentration shows a seasonal variation: It was higher in autumn and winter and lower in summer and spring. A comparison of concentrations in precipitation in Shanghai and around the Qinshan Nuclear Power Plant reveals no correlation,implying that the nuclear power plant operations may not affect the environment of Shanghai. Thus, the raised tritium concentrations in Shanghai might be due to the effects of monsoons, spring leak, raindrop, or other activities that generate tritium there. Those activities may include chemistry research that uses tritium as a tracer.     

微机在核物理实验应用中的抗干扰问题

本文简单介绍了计算机在核物理技术应用中的各种噪声，并初步探讨了抑制噪声的方法。     

Tritium concentrations in precipitation in Shanghai

Beamline BL17 U1 at Shanghai Synchrotron Radiation Facility is an energy-tunable macromolecular crystallography beamline that has been in user operation since 2009. Growing demand from the user community for a small beam and related experimental methods have motivated upgrades of the devices in the endstation.Minibeam modes have already been developed for operation. A self-integrated diffractometer reduces the sphere of confusion of the rotatory axis to 1μm. The new diffractometer is equipped with an upgraded on-axis viewing system that can improve the resolving power. Additionally,the area detector was also upgraded to the newest generation of detectors, the EIGER X 16 M, which can collect data at 133 Hz. After these upgrades, the endstation became virtually new. This paper covers the upgrade of the endstation devices and gives the first data collection results.     

2010年的美国铀矿业

2010年,美国铀矿总共施工7 209个钻孔,总进尺1 493 520 m;生产铀1 628.55t;铀矿业总支出费用为2.773亿美元,其中铀矿地勘费支出为3 450万美元,占铀矿业总费用的12.44％.铀矿地勘钻探费用为4 460万美元,占铀矿业总费用的16.08％.     

我国东南沿海城市地下建筑氡浓度分布

为了解东南沿海城市地下建筑氡浓度的分布，用固体核径迹法(SSNTD’s)，分别在春、夏、冬3季对沿海7城市地下建筑室内氡浓度进行调查。结果表明，福州具有最高的平均氡浓度，上海的平均氡浓度最低。季节的变化对地下建筑室内氡浓度有影响，各城市氡浓度平均值夏季最高、冬季最低。各城市夏季氡浓度与该城市的年均值的比值与城市中各测点氡浓度之间的离散度有一定的相关性。夏季地下建筑室内氡浓度高的城市，它的平均氡浓度受某些具有高氡水平测点的影响大。     

Plutonium use in nuclear power in Russia

Conclusions The following concept of plutonium utilization based on the evolutionary development of the traditional technology in our country arises: The main problem of any short-term program of dealing with plutonium must be solved — reliable and safe storage of separated energy plutonium and freed weapons plutonium before utilization in reactors. Plutonium (mainly energy plutonium) is utilized primarily in BN-800 fast reactors and the development of technology using weapons plutonium in BN-600 reactors starts. In the future attention should be focused on nuclear-power centers patterned after the Industrial Association “Mayak” (RT-1 plant, Complex 300, BN-800) with reliable nonproliferation of weapons plutonium. It is extremely important to speed up work on the completion of Complex 300: This work must be completed before BN-800 is ready. In the future efforts must be concentrated on the following: development and implementation, in BN-800, of an economically more efficient plutonium-burning core; the possibility of building light-water reactors with the required degree of safety for effective plutonium utilization must be justified (including a “cold” core based on cermet fuel); and, development and implementation of technology for a safe and an ecologically acceptable closed nuclear fuel cycle based on plutonium and²³³U with burnout of Am, Np, and Cm. Ministry of Atomic Energy of the Russian Federation. Institute of Physics and Power Engineering. A. A. Bochvar All-Union Scientific-Research Institute of Standardization in Machine Building. Special Design Office for Machines. Translated from Atomnaya énergiya, Vol. 76, No. 4, pp. 326–332, April, 1994.