Development of Generator Produced Positron Emitting Radionuclide Containing Diagnostic Radiopharmaceutical

为促进正电子放射性核素（P-RI）的发展，我们致力于建立正电子放射性核素（P-RI）发生器生产系统，并开发P-RI标记药物，用于肿瘤和心脑疾病的诊断。62-Cu、68-M、82-Rb和52 m-Mn发生器引起了我们的兴趣，但从国际竞技场的进展来看，1）62-Cu发生器系统，2）62-Cu和3）68-Ga标记诊断剂的开发更是迫在眉睫。1）~（62）Cu发生器系统的制备：首先以天然铜为靶进行~（63）Cu（p，2n）~（62）Zn核反应，然后探索~（62）Cu子体与~（62）Zn母体的分离方法。在研究了各种分析条件后，以62-Ci-甘氨酸络合物的形式洗脱子体使得能够实现实用的发生器系统 关于我们 茎用于生产高纯度和高产率的62-Cu。2）62-Cu标记的诊断剂：基于二缩氨基硫脲（dithiosemicarbazone，DITR）与62-Cu形成高度稳定、紧密和不变的络合物的能力，该分子被用于设计双功能螯合剂，例如，62-Cu标记的白蛋白，62-Cu标记长链脂肪酸（心肌代谢功能诊断）、62-Cu-胆甾酯衍生物（脑血流诊断）。然后，根据其未来临床应用所需的基本要求，评估每种开发的试剂在感兴趣的组织或器官中的累积机制。3）68-Ga标记的诊断试剂：放射性标记的68-Ga-柠檬酸盐用于核医学中的肿瘤诊断需要一些基础研究，以使其在短半衰期内特异性累积。此外，一些体外和体内研究与68-Ga标记的肿瘤抗体，其合理的核医学的使用正在进行中。总之，每个结果集在一起的未来发展的途径。少

To promote the expansion of Position Nuclear Medicine,our attention was focused in the establishment of generator production system for position emitting radiometallic nuclide (P-RI) and in the development of P-RI labeled pharmaceuticals for the diagnosis of tumor and brain, heart disorders . At first, 62-Cu, 68-M, 82-Rb and 52m-Mn generators attracted our interest, however, according to progress in the international arena, the development of 1) 62-Cu generator system, 2) 62-Cu and 3) 68-Ga labeled diagnostic agents occupies more imminent place. On those basis, the results are described below as follows:1) Production of 62-Cu generator system : at first, the 63-Cu (p, 2n) 62-Zn nuclear reaction using natural copper as the target was carried out; then, a separation methodology for the 62-Cu daughter from its 62-Zn parent was surveyed. After studying various analytical conditions, the elution of the daughter as the 62-Ci-glycine complex enabled the achievement of a practical generator sy … More stem for the production of of 62-Cu with high purity and high yield.2) 62-Cu labeled diagnostic agent: based on the ability of dithiosemicarbazone (DTS) to render highly stable, compact and unchanged complex with 62-Cu, this molecule was used for the design of bifunctional chelating agents, such as, the 62-Cu labeled albumin, 62-Cu labeled long chain fatty acids (function diagnosis of myocardium metabolism), 62-Cu-DTS-esther derivatives (cerebral blood flow diagnosis). Then, the accumulation mechanism of each developed agent in the tissue or organ of interest was evaluated according, to the basic,requirement needed for their future clinical applicability.3) 68-Ga labeled diagnostic agent: the use of radiolabeled 68-Ga-citrate for the tumor diagnosis in Nuclear Medicine calls for some basic studies enabling its specific accumulation within the short half-life. Also, some in-vitro and in-vivo studies with 68-Ga labeled tumor antibodies for its plausible use in Nuclear medicine is under progress.In conclusion, each result set together the pathway for future development. Less