Rhenium labeled McAb—SZ39 and colloid

Two kinds of rhenium labeled radiopharmaceuticals for therapy of the human brain glioma were prepared.Anti-human brain glioma monoclonal antibody (McAb-SZ39) was directly labeled with 186 ReO4^-.When ascorbic acid was used as reduction agent of antibody and the reduction of 186 ReO4^- was finished in sodium gluconate solution(pH=2.54),the labeling efficiency was 96.2%,After purification,the labeled products were tested in respect of immunoreactivity,in vitro stability as well as inhibitory efficiency against human glioma transplanted in nude mice,188ReO4^- labeled colloid was synthesized by using a two-step method.The size of radiocolloid particles was around 2-5μm,and the radiochemical yield was over 95%,Nude mice Experiments demonstrated that the inhibitory efficiency against human brain glioma of 188Re-collied and ^188 Re-McAb-SZ39 was 90% and 65% ,respectively.     

回旋加速器制备放射性氯化亚铊(~(201)Tl)注射液

本文叙述制备放射性氯化亚铊(~(201)Tl)注射液的方法。靶子为高纯金属铊片,装于具有水冷、气冷腔的2π靶室内,利用扇形聚焦回旋加速器所产生的30MeV质子进行辐照。靶片溶解后,联合使用液-液萃取和阴离子交换法进行化学处理,可同时获得无载体~(203)Pb。产品~(201)Tl核纯度大于99％(~(200)Tl～0.76％,~(202)Tl～0.04％),放化纯度大于98％,含铊量小于0.27×10~(-7)μg/Bq(1.0μg/mCi)~(201)Tl。化学杂质Fe、Al等均小于1ppm,~(201)Tl厚靶产额约为18.8MBq/μAh。产品经临床前药理试验、药检试验和临床试用,质量良好。     

Kiss1R Identification and Biodistribution Analysis Employing a Western Ligand Blot and Ligand-Derivative Stain with a FITC-Kisspeptin Derivative

It is not always easy to establish specific antibodies against receptors. Most receptors are hydrophobic and have complicated three-dimensional structures, making them difficult to use as immunogens. Thus, we developed receptor detection methods with a fluorescein-labeled ligand as an antibody alternative, which we referred to as a western ligand blot (WLB) and ligand derivative stain (LDS). Kisspeptin receptor (Kiss1R) was detected by its ligand. Kiss1R expression was confirmed in eight human cell lines by the WLB and in four pathological tissues by the LDS. Next, Kiss1R was stained by LDS in organs, revealing Kiss1R expression by [⁶⁷Ga]Ga-DOTA-kisspeptin 10 accumulation. As a result, Kiss1R-expressing cells in each organ could be stained with fluorescein-labeled kisspeptin 14 instead of an antibody and observed by light microscopy. The combination of the WLB and LDS allows identification of receptors in tissues, which can be readily applied to target receptor detection by a synthetic ligand derivative.     

Development of a new software for comprehensive management and traceability of hospital radiopharmacies

A database software application for comprehensive management and traceability of hospital radiopharmacies has been developed and implemented. This software is a customizable shareware called Radiolab, which provides an immediate and complete traceability of all preparations, controls and radiopharmaceuticals, as well as a great help in the management of reports, orders, stock and radioactive waste. Available by now in five languages (English, Spanish, French, Portuguese and Italian) this software and its manual can be downloaded from the Internet at www.radiopharmacy.net.     

血液中碘代芳香胺的蛋白游离率的计算

通过引入蛋白游离率的比较取代基常数,其定义为Ｃｆ＝ＬｏｇＥｘ／ＥＨ,计算了磺代芳香胺系列物的蛋白游离率的比较取代基常数。结果表明取代基不同,Ｃｆ数值不同。对一定的基团为常数,且具有加和性。该结果可用于评价药物取代基对蛋白游离率的贡献和药物的药效,以及计算磺代芳香胺的Ｅｆ值。     

脑放射性药物碘代芳香胺构效关系的定量研究

根据Ｆｉｃｋ定律，假设放射性药物可以通过扩散机制穿透血脑屏障，经过对１４种碘代芳香胺放射性药物的分析，首次得到了最初脑摄取量与药物的脂溶性、蛋白质结合率和分子量之间的定量关系，这对于脑放射性药物的设计和药物最初脑摄取量的预测具有一定的意义。     

用(γ,n)反应生产放射性药物~(123)I的研究

从理论和实验上对光核反应生成放射性药物~１２３Ｉ进行了研究，给出了有关~(１２４)Ｘｅ（γ，ｎ）~(１２３)Ｘｅ→~(１２３)Ｉ的理论计算公式和计算结果。描述了利用合肥国家同步辐射实验室２００ＭｅＶ电子直线加速器的束流和在其末端建立的实验装置。文中给出了实验得到的反应产物的放射性活度、γ射线的谱图以及化学纯度分析结果。实验结果表明：若用纯的~(１２４)Ｘｅ进行生产，在该加速器上经两个半小时照射，将可得到１８．５ＧＢｑ以上的~(１２３)Ｉ药物。     

心、脑显像剂~(99)Tc~mN-MDTC的制备及生物分布

制备了一种９９Ｔｃｍ心、脑显像剂——二硫代肼甲酸甲酯锝氮配合物（９９ＴｃｍＮ－ＭＤＴＣ），并研究了该标记化合物在小鼠体内的生物分布。结果表明，此配合物在心、脑中均有一定浓集，并有很好的滞留性质。     

多巴胺D2受体显像剂99Tcm-mEBZM生物学评价

将ECD(L,L-ethyl cysteinate dimer)分子与对多巴胺D2受体具有较高亲和力的苯酰胺分子(BZM)偶联,制备99Tcm-mEBZM,并研究了99Tcm-mEBZM在大鼠和小鼠体内的生物分布.结果显示,99Tcm-mEBZM具有较高的体外稳定性和较高的脂溶性,在小鼠的生物分布中呈现较高的进脑量(2 min时为2.97%ID@g-1),小鼠与大鼠的纹状体/小脑比值可达到1.55,提示标记物与纹状体的结合具有特异性.