【摘要】 用氯胺-T法制备了四种神经多巴胺受体显像剂:¹³¹I-IBZM,¹³¹I—IBZP,¹³¹I-ISPD和¹³¹I-ICDM其中,SPD和CDM是中药延胡索乙素的衍生物.已被证明是新型的DA阻滞剂。本文首次报道了其碘标记物的制备。研究了影响标记产额的因素。为了得到高比活度标记物,使用反相HPLC法对标记物及其前体进行了分离,对如何选择HPLC分离条件及制备过程的产额做了研究和讨论。更多还原

【Abstract】 To develop new specific receptor-site brain imaging agents labeled with radioiodine for Single Photo Emisson Computed Tomagraphy（SPECT）, Four potential’DA receptor imaging agents,¹³¹I-labeled IBZM, IBZP, ISPD and ICDM have been prepared from corresponding uniodinated compounds. Among them SPD and CDM are analogs of L-tetrahydropεlmatine, which is the main component of Corydlis,a traditional Chinese medicine, and have both been demonstrated to be a new type of DA receptor antagonists. Using Chloramine-T as oxidant and in pH=3phosphate buffer, over 80% labeling yield was obtained at room temperature. As unlabeled precursors are similar to the radioiodinated products in chemical structures and biological behavior, very efficient purification techniques are required. We uselreverse HPLC to separate labeled products from unlabeled impuritiec. With suitable pH buffer and solvent, we got satisfactory column selectivity and resolution with optimal separation conditions. After labeling vnd HPLC purification, the overall yield was 20—40%.更多还原