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[18F]3F4AP的自动化放射化学合成:一种用于成像脱髓鞘疾病的新型正电子发射断层显像(PET)示踪剂

Automated Radiochemical Synthesis of [18F]3F4AP: A Novel PET Tracer for Imaging Demyelinating Diseases.

作者信息

Brugarolas Pedro, Bhuiyan Mohammed, Kucharski Anna, Freifelder Richard

机构信息

Department of Neurology, The University of Chicago;

Department of Radiology, The University of Chicago.

出版信息

J Vis Exp. 2017 May 29(123):55537. doi: 10.3791/55537.

Abstract

3-[F]fluoro-4-aminopyridine, [F]3F4AP, is a radiofluorinated analog of the FDA-approved drug for multiple sclerosis 4-aminopyridine (4AP). This compound is currently under investigation as a PET tracer for demyelination. We recently described a novel chemical reaction to produce metafluorinated pyridines consisting of direct fluorination of a pyridine N-oxide and the utilization of this reaction for the radiochemical synthesis of [F]3F4AP. In this article, we demonstrate how to produce this tracer using an automated synthesizer and an in-house made flow hydrogenation reactor. We also show the standard quality control procedures performed before releasing the radiotracer for preclinical animal imaging studies. This semi-automated procedure may serve as the basis for future production of [F]3F4AP for clinical studies.

摘要

3-[F]氟-4-氨基吡啶([F]3F4AP)是美国食品药品监督管理局(FDA)批准用于治疗多发性硬化症的药物4-氨基吡啶(4AP)的放射性氟化类似物。该化合物目前正作为一种用于脱髓鞘的正电子发射断层显像(PET)示踪剂进行研究。我们最近描述了一种制备间位氟化吡啶的新化学反应,该反应包括吡啶N-氧化物的直接氟化,并将此反应用于[F]3F4AP的放射化学合成。在本文中,我们展示了如何使用自动合成仪和自制的流动氢化反应器来制备这种示踪剂。我们还展示了在将放射性示踪剂用于临床前动物成像研究之前所执行的标准质量控制程序。这种半自动程序可为未来用于临床研究的[F]3F4AP的生产奠定基础。

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