在相转移催化下从MLN-4760的F/Cl交换中获得的ACE2 PET成像剂
Pan Zhou1,2, Kai Ning3, Shuai Xue2
1Department of Nuclear Medicine, Shanghai Changhai Hospital, Shanghai, 200433, China.
EJNMMI radiopharmacy and chemistry
|December 2, 2024
概括
研究人员开发了一种新的放射性标记物,18F-MLN-4760,用于成像 ангиотензин转化酶-2 (ACE2). 这种标记器显示了高ACE2表达的器官的特定向和吸收,证明了其用于诊断成像的潜力.
科学领域:
- 放射化学和分子成像技术
- 生物医学研究生物医学研究
- 药理学 药理学是指药理学的学科.
背景情况:
- ангиотензин转化酶-2 (ACE2) 在病理重塑和治疗点中至关重要.
- 开发有效的ACE2成像剂对于疾病诊断和监测至关重要.
研究的目的:
- 为了合成和评估一种新型的18F标记的MLN-4760放射性联体,用于ACE2向的PET成像.
- 在人性化的ACE2小鼠模型中研究18F-MLN-4760的准能力和生物分布.
主要方法:
- 使用催化式18F换Cl (18F/Cl) 交换方案的快速合成路线被采用.
- 18F-MLN-4760使用SepPak C18列进行了合成和净化.
- 在一个人性化的ACE2小鼠模型中进行了正子发射断层扫描 (PET) 成像和生物分布研究.
主要成果:
- 18F-MLN-4760成功合成,放射性化学产量为30%,纯度为29.89%.
- PET成像显示18F-MLN-4760在具有高ACE2表达的器官中的特定吸收和良好的稳定性.
- 生物分布数据和免疫组织化学证实了对过度表达ACE2的组织的高特异性,吸收和ACE2水平之间存在强烈的相关性 (r=0.935).
结论:
- 18F-MLN-4760在相转移催化下通过18F/Cl交换有效合成.
- 放射性体表现出高特异性和与ACE2表达水平的良好相关性.
- 18F-MLN-4760显示出作为潜在的PET成像探头的承诺,用于准ACE2.
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