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发明授权
CN101537193B 一种囊泡单胺转运体靶向结合药物及其制备方法 失效 - 权利终止

一种囊泡单胺转运体靶向结合药物及其制备方法
摘要：
本发明涉及一种囊泡单胺转运体靶向结合药物及其制备方法，其中所含的显像剂的结构如下：其中，R1＝H，-CH3，-CH2CH3；R2＝-(CH2)n-F，n＝1～4，-(CH2CH2O)nCH2CH2-F，n＝1～3。本发明以TBZ为先导化合物，将TBZ的2位羰基换成氨基，设计合成系列新的含F的TBZ-NH2衍生物，该系列TBZ-NH2衍生物一方面具有较高的靶向性，可以与VMAT2特异性结合；另一方面当用F-18代替F-19时，可以用于PET显像研究，是具有良好应用前景的PD诊断显像剂和糖尿病诊断显像剂。
摘要（英）：

The invention relates to a vesicle monoamine transporter target bound drug and a preparation method thereof; wherein the structure of a contained developing agent is shown as right; wherein R1=H, -CH3, -CH2CH3; R2=-(CH2)n-F, n=1-4, -(CH2CH2O)nCH2CH2-F, n=1-3. The invention adopts TBZ as lead compound, replaces 2-carbonyl group of TBZ with amino group and designs to synthetize a series of new TBZ-NH2 derivatives containing F; the series of TBZ-NH2 derivatives not only has higher targeting property and can be combined the specificity of VMAT2, but also can be used for PET development research when using F-18 to replace F-19, and is a developing agent which is used for PD diagnosis and diabetes diagnosis and has a good application prospect.

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