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使用通用电气TRACERlab FXC-Pro全自动合成用于18 kDa转位蛋白(TSPO)的放射性药物[¹¹C]PBR28。

Fully automated radiosynthesis of [¹¹C]PBR28, a radiopharmaceutical for the translocator protein (TSPO) 18 kDa, using a GE TRACERlab FXC-Pro.

作者信息

Hoareau Raphaël, Shao Xia, Henderson Bradford D, Scott Peter J H

机构信息

Department of Radiology, University of Michigan, Ann Arbor, MI 48109, USA.

出版信息

Appl Radiat Isot. 2012 Aug;70(8):1779-83. doi: 10.1016/j.apradiso.2012.03.006. Epub 2012 Mar 29.

Abstract

In order to image the translocator protein (TSPO) 18kDa in the clinic using positron emission tomography (PET) imaging, we had a cause to prepare [(11)C]PBR28. In this communication we highlight our novel, recently developed, one-pot synthesis of the desmethyl-PBR28 precursor, as well as present an optimized fully automated preparation of [(11)C]PBR28 using a GE TRACERlab FX(C-Pro). Following radiolabelling, purification is achieved by HPLC and, to the best of our knowledge, the first reported example of reconstituting [(11)C]PBR28 into ethanolic saline using solid-phase extraction (SPE). This procedure is operationally simple, and provides high quality doses of [(11)C]PBR28 suitable for use in clinical PET imaging studies. Typical radiochemical yield using the optimized method is 3.6% yield (EOS, n=3), radiochemical and chemical purity are consistently >99%, and specific activities are 14,523Ci/mmol.

摘要

为了在临床上使用正电子发射断层扫描(PET)成像对18kDa的转运蛋白(TSPO)进行成像,我们有理由制备[(11)C]PBR28。在本通讯中,我们重点介绍了我们新颖的、最近开发的去甲基-PBR28前体的一锅法合成,以及使用GE TRACERlab FX(C-Pro)对[(11)C]PBR28进行优化的全自动制备方法。放射性标记后,通过高效液相色谱法进行纯化,据我们所知,这是首次报道使用固相萃取(SPE)将[(11)C]PBR28重构成乙醇盐水的例子。该方法操作简单,可提供适用于临床PET成像研究的高质量[(11)C]PBR28剂量。使用优化方法的典型放射化学产率为3.6%(EOS,n = 3),放射化学和化学纯度始终>99%,比活度为14,523Ci/mmol。

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