In-LOOP synthesis of <sup>11</sup>C-Triphenylmethylphosphonium for myocardial perfusion imaging

SUN Huiping1 ZHOU Weihua1 ZHANG Jinmin2 ZHANG Xiaojun2 LIU Jian2 TIAN Jiahe2 1

doi:10.11889/j.0253-3219.2013.hjs.36.020303

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In-LOOP synthesis of ¹¹C-Triphenylmethylphosphonium for myocardial perfusion imaging

更新时间：2021-06-03

- In-LOOP synthesis of ¹¹C-Triphenylmethylphosphonium for myocardial perfusion imaging
- NUCLEAR TECHNIQUES Vol. 36, Issue 2, Article number: 020303(2013)
- 作者机构：
  
  1. 中国人民武装警察总医院
  2. 中国人民解放军总医院
- 作者简介：
- 基金信息：
- DOI：10.11889/j.0253-3219.2013.hjs.36.020303
  CLC： R914
- Published：2013
- 稿件说明：
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[1]孙慧萍,周卫华,张锦明,张晓军,刘健,田嘉禾.在线合成心肌灌注显像剂:碳-11三苯甲基磷[J].核技术,2013,36(02):53-57.

SUN Huiping1 ZHOU Weihua1 ZHANG Jinmin2 ZHANG Xiaojun2 LIU Jian2 TIAN Jiahe2 1. In-LOOP synthesis of ¹¹C-Triphenylmethylphosphonium for myocardial perfusion imaging[J]. Nuclear techniques, 2013, 36(2): 020303
[1]孙慧萍,周卫华,张锦明,张晓军,刘健,田嘉禾.在线合成心肌灌注显像剂:碳-11三苯甲基磷[J].核技术,2013,36(02):53-57. DOI： 10.11889/j.0253-3219.2013.hjs.36.020303.

SUN Huiping1 ZHOU Weihua1 ZHANG Jinmin2 ZHANG Xiaojun2 LIU Jian2 TIAN Jiahe2 1. In-LOOP synthesis of ¹¹C-Triphenylmethylphosphonium for myocardial perfusion imaging[J]. Nuclear techniques, 2013, 36(2): 020303 DOI： 10.11889/j.0253-3219.2013.hjs.36.020303.

摘要

99mTc-MIBI是常用的心肌灌注显像剂

肝摄取高

临床应用有一定的影响。11C-三苯甲基磷（11C-TPMP）为脂溶性正一价阳离子

用于心肌显像能得到更好的分辨率。以11CH3-Triflate为甲基化试剂

采用LOOP法在线合成了11C-TPMP

研究了11C-TPMP在正常小鼠的分布

正常大鼠行Micro PET显像

并与4位18F-苯基三苯基磷（18F-FTPP）比较。结果显示

LOOP法合成11C-TPMP效率大于90%（校正）

放化纯度大于98%。正常小鼠心肌有高的摄取

注射后5 min和60 min

心肌摄取分别为（71.9±19.9）%ID.g–1和（12.87±0.81）%ID.g–1

肝摄取低

注射后5 min和60 min心肝摄取比分别为11.57和3.2。正常大鼠micro PET显像显示

从20 min到60 min

心肌显像清晰

肝未显像。表明LOOP法可高效合成11C-TPMP

11C-TPMP是一个很有希望的心肌灌注显像剂。

Abstract

Background:99mTc-MIBI was used as myocardial perfusion SPECT.However

the high accumulation of tracers in the liver and lung may hinder the detection of flow abnormalities in myocardium.Purpose: 11C-Triphenylmethylphosphonium（11C-TPMP） was a lipophilic cation

has been investigated as a positron emission tomography（PET） agent for myocardial and tumor imaging to provide a better temporal and spatial resolution than SPECT.Methods: 11C-TPMP was prepared by reacting [11C]methyl trifalte with In-LOOP method.Biodistribution studies in mouse were performed.And micro PET was performed with rat

and compared with 4-[18F]fluorophenyl triphenylphosphonium ion（18F-FTPP）.Results: The results showed that the 11C-TPMP labeling yield was over 90%

the radiochemical purity was over 98%.The biodistribution showed high accumulation of radioactivity in the heart（71.9±19.9）%ID.g–1 at 5 min and（12.87±0.81）%ID.g–1at 60 min post injection.The heart/liver ratios were 11.57 and 3.2 at 5 min

60 min respectively.Micro PET scans showed distinct accumulation of 11C-TPMP in the myocardium from 20 min to 60 min.The liver had very lower accumulation of radioactivity.Conclusions: 11C-TPMP was a promise PET perfusion agent for myocardial.It would be useful in clinical with In-LOOP synthesis.

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In-LOOP synthesis of 11C-Triphenylmethylphosphonium for myocardial perfusion imaging

DOI：10.11889/j.0253-3219.2013.hjs.36.020303

摘要

Abstract

关键词

Keywords

references

In-LOOP synthesis of ¹¹C-Triphenylmethylphosphonium for myocardial perfusion imaging