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自动化合成腺苷 A 受体靶向放射性示踪剂 [ F]FLUDA。

Automated radiosynthesis of the adenosine A receptor-targeting radiotracer [ F]FLUDA.

机构信息

Department of Neuroradiopharmaceuticals, Institute of Radiopharmaceutical Cancer Research, Helmholtz-Zentrum Dresden-Rossendorf, Leipzig, Germany.

Department of Research and Development, ROTOP Pharmaka GmbH, Dresden, Germany.

出版信息

J Labelled Comp Radiopharm. 2022 May 30;65(6):162-166. doi: 10.1002/jlcr.3970. Epub 2022 Mar 24.

Abstract

[ F]FLUDA is a selective radiotracer for in vivo imaging of the adenosine A receptor (A R) by positron emission tomography (PET). Promising preclinical results obtained by neuroimaging of mice and piglets suggest the translation of [ F]FLUDA to human PET studies. Thus, we report herein a remotely controlled automated radiosynthesis of [ F]FLUDA using a GE TRACERlab FX2 N radiosynthesizer. The radiotracer was obtained by a one-pot two-step radiofluorination procedure with a radiochemical yield of 9±1%, a radiochemical purity of ≥99%, and molar activities in the range of 69-333 GBq/μmol at the end of synthesis within a total synthesis time of approx. 95 min (n = 16). Altogether, we successfully established a reliable and reproducible procedure for the automated production of [ F]FLUDA.

摘要

[F]FLUDA 是一种用于正电子发射断层扫描(PET)体内成像的腺苷 A 受体(A R)的选择性放射性示踪剂。通过对小鼠和仔猪进行神经影像学研究获得了有前景的临床前结果,这表明 [F]FLUDA 可以转化为人类 PET 研究。因此,我们在此报告了使用 GE TRACERlab FX2 N 放射性合成器进行的 [F]FLUDA 的远程控制自动化放射性合成。该放射性示踪剂通过一锅两步放射性氟化程序获得,放射性化学产率为 9±1%,放射性化学纯度≥99%,摩尔活度在合成结束时在 69-333GBq/μmol 范围内,总合成时间约为 95min(n=16)。总之,我们成功建立了一种可靠且可重复的 [F]FLUDA 自动化生产程序。

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