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目的研制早期诊断帕金森病的多巴胺转运蛋白（ＤＡＴ）显像剂９９Ｔｃｍ２β［Ｎ，Ｎ′双（２巯乙基）乙撑二胺基］甲基，３β（４氯苯基）托烷（ＴＲＯＤＡＴ１）。方法以可卡因为原料，经多步反应，合成配体ＴＲＯＤＡＴ１；用亚锡作还原剂，在葡庚糖酸钠（ＧＨ）存在下制备９９ＴｃｍＴＲＯＤＡＴ１。测定标记物的稳定性及在磷酸缓冲液和正辛醇中的分配系数，进行大鼠体内分布和猴显像实验。结果经ＩＲ、１ＨＮＭＲ、ＭＳ等鉴定，ＴＲＯＤＡＴ１与结构一致。制备的９９ＴｃｍＴＲＯＤＡＴ１经ＨＰＬＣ测定其放化纯＞９０％，室温下放置２４ｈ稳定；ｐＨ值７０和７４时的分配系数分别为１３２和１５４。大鼠体内分布结果：９９ＴｃｍＴＲＯＤＡＴ１在脑内浓聚较低（２、６０ｍｉｎ分别为０２８％和０１２％ＩＤ／ｏｒｇａｎ），但脑纹状体摄取２、３０、６０、１２０ｍｉｎ分别为０１９３％、０１８９％、０１４２％和０１３６％ＩＤ／ｇ，保留很好；而小脑、大脑皮质和海马清除较快，纹状体与小脑的比值随时间延长而升高（２、３０、６０、１２０ｍｉｎ分别为１０６、１７７、２４０和４４５），１２０ｍｉｎ纹状体与海马和大脑皮质的比值分?
Objective To develop a dopamine transporter (DAT) imaging agent for the early diagnosis of Parkinson’s disease, 99Tcm2β [N, N’bis (2mercaptoethyl) ethylenediamino] methyl, 3β Phenyl) tropane (TRODAT 1). Methods Cocaine as a raw material, after a multi-step reaction, the synthesis of ligand TRODAT 1; with stannous as a reducing agent, in the presence of glucoheptonate (GH) Preparation 99Tcm TRDAT 1. The stability of the label and the partition coefficient in phosphate buffer and n-octanol were measured to determine the distribution in vivo and the monkey imaging experiment in rats. The results of IR, 1HNMR, MS identification, TRODAT 1 consistent with the structure. Preparation of 99Tcm TRODAT 1 determined by HPLC radioactive purity> 90%, 24h standing at room temperature stability; pH 7 0 and 7 4 when the partition coefficient of 132 and 154, respectively. In vivo distribution results: 99Tcm TRODAT 1 in the brain less concentrated (2,60 min were 028% and 0 12% ID / organ), but the brain striatum uptake 2,30,60, 120min were 0 193%, 0 189%, 0 142% and 0 136% ID / g, retained well; and cerebellum, cerebral cortex and hippocampus cleared faster, striatum and cerebellum ratio over time (2,30,60,120 min respectively 1 06,1 77,2 40 and 4 45), 120min striatum and hippocampus and cerebral cortex ratio score?