Synthesis and evaluation of serotonin transporter imaging agent [<sup>125</sup>I]-ADAM

JIANG Quanfu WU Chunying LU Chunxiong CHEN Zhengping WANG Songpei ZHANG Tongxing LI Xiaomin ZHU Junqing

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Synthesis and evaluation of serotonin transporter imaging agent [¹²⁵I]-ADAM

更新时间：2021-03-12

- Synthesis and evaluation of serotonin transporter imaging agent [¹²⁵I]-ADAM
- NUCLEAR TECHNIQUES Issue 10, (2005)
- 作者机构：
  
  1. 江苏省原子医学研究所卫生部核医学重点实验室
  2. 江苏省原子医学研究所卫生部核医学重点实验室,无锡,214063
- 作者简介：
- 基金信息：
  
  江苏省“135”医学重点人才基金(RC2002068);江苏省“六大人才高峰”基金(2003-07)资助
- DOI：
  CLC： R817
- Published：01 October 2005
- 稿件说明：
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[1]蒋泉福,吴春英,陆春雄,陈正平,王颂佩,张同兴,李晓敏,朱钧清.5-羟色胺转运体显像剂[~(125)I]-ADAM的合成以及初步生物学分布[J].核技术,2005(10):766-770.

JIANG Quanfu WU Chunying LU Chunxiong CHEN Zhengping WANG Songpei ZHANG Tongxing LI Xiaomin ZHU Junqing. Synthesis and evaluation of serotonin transporter imaging agent [¹²⁵I]-ADAM[J]. Nuclear techniques, 2005, (10): 766-770.
[1]蒋泉福,吴春英,陆春雄,陈正平,王颂佩,张同兴,李晓敏,朱钧清.5-羟色胺转运体显像剂[~(125)I]-ADAM的合成以及初步生物学分布[J].核技术,2005(10):766-770. DOI：

JIANG Quanfu WU Chunying LU Chunxiong CHEN Zhengping WANG Songpei ZHANG Tongxing LI Xiaomin ZHU Junqing. Synthesis and evaluation of serotonin transporter imaging agent [¹²⁵I]-ADAM[J]. Nuclear techniques, 2005, (10): 766-770. DOI：

摘要

完成了5-羟色胺转运体显像剂[125I]-2-（（2-（（二甲基氨基）甲基）苯基）巯基）5-碘苯胺（[125I]-2-（（2-（（dimethylamino）methyl）phenyl）thio）-5-iodophenylamine

[125I]ADAM）的制备和初步生物学特性的评价。以2

5-二溴-硝基苯和2-巯基苯甲酸为起始原料

合成标记前体5-三丁基锡-2-[2-（二甲基氨基甲基苯基巯基）]苯胺

采用双氧水标记法标记;并进行了大鼠体内和脑内的初步生物分布研究。合成标记前体5-三丁基锡-2-[2-（二甲基氨基甲基苯基巯基）]苯胺的总产率为42%

用[125I]NaI标记后

TLC测放射化学纯度（RCP）大于95%;125I-ADAM大鼠脑摄取高

在富含5-羟色胺转运蛋白的丘脑中的摄取随时间延长而增加

滞留时间长

其特异结合在注射后60min、120min和240min分别为3.38

3.62和4.36。本合成方法总收率高

标记方法简便

放射化学纯度高

125I-ADAM初始进脑量高

与SERT结合特异

可望用于研究脑内SERT功能。

Abstract

Synthsis of a new ligand: 2-((2-((Dimethylamino)methyl)phenyl)thio)-5–iodophenylamine(125I-ADAM) as a serotonin imaging agent is reported. The radioiodinated ligand was prepared by iododestannylation reaction using hydrogen peroxide. The chemical structure of the labeling precursor (5-(tributylstannyl)-2-((2-((dimethylamino) methyl)phenyl)thio)phenylamine) and all intermediates were verified by IR

HNMR and MS. The radiochemical purity of 125I-ADAM was above 95% determined by TLC. Biodistribution studies in rats showed that the initial uptake of 125I-ADAM in the brain was high

and consistently the highest binding appeared in hypothalamus

a region with the highest density of SERT. The specific binding ((T/CB)-1) of 125I-ADAM in hypothalamus were 3.38

3.62 and 4.36 at 60 min

120 min and 240 min postinjection

respectively. These data suggest that 125I-ADAM may be useful for SPECT imaging of SERT binding sites in the brain.

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Synthesis and evaluation of serotonin transporter imaging agent [125I]-ADAM

DOI：

摘要

Abstract

关键词

Keywords

references

Synthesis and evaluation of serotonin transporter imaging agent [¹²⁵I]-ADAM