多巴胺D2受体显像剂125I-DMAIBZM的合成及生物分布实验

为提高苯甲酰胺类衍生物（S）-N-（1-乙基-2-吡咯烷基）甲基-4-氨基-2-甲氧基苯酰胺（ABZM）的入脑量，对其结构进行改造，得到了新的化合物（S）-4-二甲氨基-N-（1-乙基-2-吡咯烷基）甲基-2-甲氧基苯酰胺（DMABZM）.通过Idogen法对DMABZM进行标记得到标记化合物125I-DMAIBZM，标记率为74%，放化纯度达到99%． 体外放射配基结合实验测得DMABZM的IC50为2.9589×10-7 mol?L-1，表明它与能与多巴胺D2受体特异性结合且具有较高的亲和力，在小鼠体内的分布实验中，该标记物纹状体/小脑的比值可达6.5左右，说明了该标记化合物与纹状体的结合有较高的特异性和亲和力．125I-DMAIBZM的脂溶性显著大于125I-AIBZM，入脑量有较大的提高．结论：125I（123I）-DMAIBZM有望用于多巴胺D2受体的显像．

Synthesis and Biodistribution of ~(125)I-DMAIBZM for Dopamine D2 Receptor Imaging

Many kinds of central nervous system diseases,such as Parkinson's disease,have great relationship with abnormality of cerebral dopaminergic neurotransmission.Radioactive brain receptor imaging technique can be used to acquire the information of dopamine receptor to infer the situation of dopamine.(S)-5-125I-N-(1-Ethyl-2-pyrrolidinyl)methyl-4-amine-2-methoxy-benzamide(125I-AIBZM) shows high binding affinity with dopaminergic receptor;however,the application of 125I-AIBZM is limited for its low brain biodistr...