Automated radiosynthesis and preliminary animal experiments of (S-[<sup>11</sup>C]-methyl)-D-cysteine

LIANG Xiang WANG Hongliang HUANG Tingting TANG Ganghua HU Kongzhen WU Kening

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Automated radiosynthesis and preliminary animal experiments of (S-[¹¹C]-methyl)-D-cysteine

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- Automated radiosynthesis and preliminary animal experiments of (S-[¹¹C]-methyl)-D-cysteine
- NUCLEAR TECHNIQUES Vol. 35, Issue 6, (2012)
- 作者机构：
  
  中山大学附属第一医院核医学科
- 作者简介：
- 基金信息：
  
  国家863计划基金(2008AA02Z430);国家自然科学基金(30970856);国际原子能机构(IAEA)基金(15245/R0);教育部留学回国启动基金(教外司留[2010]609号)资助
- DOI：
  CLC： R817.4
- Published：01 January 4
- 稿件说明：
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[1]梁祥,王红亮,黄婷婷,唐刚华,胡孔珍,吴克宁.(S-[~(11)C]甲基)-D-半胱氨酸的自动合成与动物实验[J].核技术,2012,35(06):452-456.

LIANG Xiang WANG Hongliang HUANG Tingting TANG Ganghua HU Kongzhen WU Kening. Automated radiosynthesis and preliminary animal experiments of (S-[¹¹C]-methyl)-D-cysteine[J]. Nuclear techniques, 2012, 35(6): 452-456.
[1]梁祥,王红亮,黄婷婷,唐刚华,胡孔珍,吴克宁.(S-[~(11)C]甲基)-D-半胱氨酸的自动合成与动物实验[J].核技术,2012,35(06):452-456. DOI：

LIANG Xiang WANG Hongliang HUANG Tingting TANG Ganghua HU Kongzhen WU Kening. Automated radiosynthesis and preliminary animal experiments of (S-[¹¹C]-methyl)-D-cysteine[J]. Nuclear techniques, 2012, 35(6): 452-456. DOI：

摘要

研究（S-[11C]甲基）-D-半胱氨酸（11C-D-MCYS）的自动化合成工艺

并对无菌炎症模型和S180肉瘤模型进行正电子发射断层（PET）显像。由PET回旋加速器生产的11CO2

与氢化铝锂（LiAlH4）发生还原反应生成11CH3OH

再与氢碘酸（HI）发生取代反应生成碘甲烷（11CH3I）。11CH3I与前体D-半胱氨酸（D-CYS）在Sep Pak Plus C18柱上发生烷基化反应生成11C-D-MCYS。用NaH2PO4缓冲液将柱上的11C-D-MCYS淋洗到无菌瓶中。11C-D-MCYS未校正放化产率为（51±4）%（从11CH3I计算

n=4）

放化纯度

99%

总合成时间

2 min。PET显像结果显示

S180肉瘤组织高度摄取11C-D-MCYS

而炎症组织摄取11C-D-MCYS低

表明11C-D-MCYS在肿瘤显像方面具有一定潜力。

Abstract

In this work

we investigated the feasibility of automated synthesis of(S-[11C]-methyl)-D-cysteine(11C-D-MCYS) as positron emission tomography tracer for tumor imaging.11CH3I was prepared by substitution reaction of HI with 11CH3OH

which was obtained from the reaction of LiAlH4 with 11CO2.11C-D-MCYS was produced by 11C-methylation of the precursor D-cysteine with 11CH3I and purification on commercial Sep Pak C18 cartridges.The uncorrected radiochemical yield of 11C-D-MCYS from 11CH3I was over(51±4)%

the radiochemical purity of 11C-D-MCYS was more than 99%

and the total synthesis time was about 12 min.PET imaging studies showed that 11C-D-MCYS had high uptake in the S180 sarcoma-bearing tissues

but low uptake in inflammatory tissues.It seems that 11C-D-MCYS is a potential PET tracer for tumor imaging.

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Related Author

王红亮

唐刚华

黄婷婷

吴克宁

LIANG Xiang WANG Hongliang TANG Ganghua HUANG Tingting WU Kening

潘栋辉

YANG Min1 WANG Guangji2 XU Yuping1 PAN Donghui1 WANG Songpei1 LI Xiaomin1 TANG Jie1 LUO Shineng1 1

王广基

Related Institution

Department of Nuclear Medicine,No.1 Hospital Affliated to Sun Yat-Sen University

中国药科大学

Jiangsu Institute of Nuclear Medicine, Key Laboratory of Nuclear Medicine, Ministry of Health, Wuxi 214063, China) 2

中国原子能科学研究院同位素研究所

北京100083 中国原子能科学研究院同位素研究所北京102413 中国同位素公司北京

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Automated radiosynthesis and preliminary animal experiments of (S-[11C]-methyl)-D-cysteine

DOI：

摘要

Abstract

关键词

Keywords

references

Automated radiosynthesis and preliminary animal experiments of (S-[¹¹C]-methyl)-D-cysteine