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99Tcm标记苯托品类多巴胺转运蛋白显像剂的制备和小鼠体内分布
引用本文:张春艳,贾红梅,贾芳,刘伯里.99Tcm标记苯托品类多巴胺转运蛋白显像剂的制备和小鼠体内分布[J].核化学与放射化学,2002,24(4):232-235.
作者姓名:张春艳  贾红梅  贾芳  刘伯里
作者单位:北京师范大学,化学系,北京,100875
基金项目:北京师范大学青年基金资助项目 ( 2 72 0 0 7)
摘    要:合成了以苯托品(Benztropine)为前体的含巯基的单齿化合物,其光谱数据和结构相符。使用配体交换法与3-硫杂-1,5-戊二硫醇(SSS)配位合成了^99Tc^m的“3+1”型混配螯合物a。螯合物a在小鼠脑中有一定的初始摄取和滞留量,在t=5min时,ID=1.03%/g;对纹状体也有一定的亲和力,纹状体和小脑摄取比值随时间延长而增加,在t=60min时,R(纹状体/小脑)=1.3。混配螯合物有成为多巴胺转运蛋白显像剂的可能。

关 键 词:标记  多巴胺转运蛋白显像剂  苯托品  生物分布  纹状体  放射性药物  锝99
文章编号:0253-9950(2002)04-0232-04
修稿时间:2002年1月25日

SYNTHESIS, LABELING AND BIODISTRIBUTION OF TECHNETIUM-99-LABELED BENZTROPINE ANALOGS AS DOPAMINE TRANSPORTER IMAGING AGENTS
ZHANG Chun-yan,JIA Hong-mei,JIA Fang,LIU Bo-li.SYNTHESIS, LABELING AND BIODISTRIBUTION OF TECHNETIUM-99-LABELED BENZTROPINE ANALOGS AS DOPAMINE TRANSPORTER IMAGING AGENTS[J].Journal of Nuclear and Radiochemistry,2002,24(4):232-235.
Authors:ZHANG Chun-yan  JIA Hong-mei  JIA Fang  LIU Bo-li
Affiliation:ZHANG Chun-yan,JIA Hong-mei,JIA Fang,LIU Bo-liDepartment of Chemistry,Beijing Normal University,Beijing 100875,China
Abstract:In developing 99Tc m-labelled dopamine transporter imaging agents, a new substituted compound is designed and synthesized. By tetering S 3 chelate system onto it, one technetium "3+1" complex is formed. Biodistribution studies are carried out in mice. The results demonstrate that the labeled compound(a) has the ability to penetrate the intergrate blood brain barrier(1.03 %/g), at 5 min, post injection and retains for a certain time in brain. The ST/CB is 1.3 at 60 min after iv injection in mice. It also shows that brain uptake and selectivity of labeled compound(a) are higher and further improving is needed.
Keywords:dopaimine transporter  99Tc  m  benztropine  biodistribution
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