Biological evaluation of 99Tcm-labeled dopamine D2 receptor imaging agent mEBZM

HAO Bin QIAN Jun GAO Xiujian SHEN Minghua MENG Laping ZHU Jianhua

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Biological evaluation of ⁹⁹Tc^m-labeled dopamine D₂ receptor imaging agent mEBZM

更新时间：2021-03-12

- Biological evaluation of ⁹⁹Tc^m-labeled dopamine D₂ receptor imaging agent mEBZM
- NUCLEAR TECHNIQUES Issue 11, (2003)
- 作者机构：
  
  1. 复旦大学药学院
  2. 复旦大学药学院,上海,200032
- 作者简介：
- 基金信息：
- DOI：
  CLC： R817
- Published：01 November 2003
- 稿件说明：
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[1]郝彬,钱隽,高秀健,沈鸣华,孟腊平,朱建华.多巴胺D_2受体显像剂~(99)Tc~m-mEBZM生物学评价[J].核技术,2003(11):841-844.

HAO Bin QIAN Jun GAO Xiujian SHEN Minghua MENG Laping ZHU Jianhua. Biological evaluation of ⁹⁹Tc^m-labeled dopamine D₂ receptor imaging agent mEBZM[J]. Nuclear techniques, 2003, (11): 841-844.
[1]郝彬,钱隽,高秀健,沈鸣华,孟腊平,朱建华.多巴胺D_2受体显像剂~(99)Tc~m-mEBZM生物学评价[J].核技术,2003(11):841-844. DOI：

HAO Bin QIAN Jun GAO Xiujian SHEN Minghua MENG Laping ZHU Jianhua. Biological evaluation of ⁹⁹Tc^m-labeled dopamine D₂ receptor imaging agent mEBZM[J]. Nuclear techniques, 2003, (11): 841-844. DOI：

摘要

将ECD（L

L-ethyl cysteinate dimer）分子与对多巴胺D2受体具有较高亲和力的苯酰胺分子（BZM）偶联

制备99Tcm-mEBZM

并研究了99Tcm-mEBZM在大鼠和小鼠体内的生物分布。结果显示

99Tcm-mEBZM具有较高的体外稳定性和较高的脂溶性

在小鼠的生物分布中呈现较高的进脑量（2 min时为2.97％ID·g-1）

小鼠与大鼠的纹状体/小脑比值可达到1.55

提示标记物与纹状体的结合具有特异性。

Abstract

99Tcm-labeled dopamine D2 receptor imaging agent 99Tcm-mEBZM was prepared and the biological evaluation was studied. ECD( L

L-ethyl cysteinate dimer) was conjugated with the benzamide derivative

which has high affinity with dopamine D2 receptor

to yield 99Tcm-mEBZM. The biodistribution of 99Tcm-mEBZM in rats and mice was studied. The results showed that 99Tcm-mEBZM has higher stability in vitro and higher lipophilicity. The brain uptake of 99Tcm-mEBZM in mice is high(2.97%ID·g-1 at 2 min)

and the ratios of striatum /cerebellum both in rats and in mice were >1.55.

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