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Microfluidic radiosynthesis and biodistribution of [18F] 2-(5-fluoro-pentyl)-2-methyl malonic acid Microfluidic radiosynthesis and biodistribution of [18F] 2-(5-fluoro-pentyl)-2-methyl malonic acid.
- Source :
- Journal of Labelled Compounds & Radiopharmaceuticals; May2013, Vol. 56 Issue 5, p289-294, 6p
- Publication Year :
- 2013
-
Abstract
- Microfluidics technology has emerged as a powerful tool for the radiosynthesis of positron emission tomography (PET) and single-photon emission computed tomography radiolabeled compounds. In this work, we have exploited a continuous flow microfluidic system (Advion, Inc., USA) for the [<superscript>18</superscript>F]-fluorine radiolabeling of the malonic acid derivative, [<superscript>18</superscript>F] 2-(5-fluoro-pentyl)-2-methyl malonic acid ([<superscript>18</superscript>F]-FPMA), also known as [<superscript>18</superscript>F]-ML-10, a radiotracer proposed as a potential apoptosis PET imaging agent. The radiosynthesis was developed using a new tosylated precursor. Radiofluorination was initially optimized by manual synthesis and served as a basis to optimize reaction parameters for the microfluidic radiosynthesis. Under optimized conditions, radio-thin-layer chromatography analysis showed 79% [<superscript>18</superscript>F]-fluorine incorporation prior to hydrolysis and purification. Following hydrolysis, the [<superscript>18</superscript>F]-FPMA was purified by C18 Sep-Pak, and the final product was analyzed by radio-HPLC (high-performance liquid chromatography). This resulted in a decay-corrected 60% radiochemical yield and ≥98% radiochemical purity. Biodistribution data demonstrated rapid blood clearance with less than 2% of intact [<superscript>18</superscript>F]-FPMA radioactivity remaining in the circulation 60 min post-injection. Most organs showed low accumulation of the radiotracer, and radioactivity was predominately cleared through kidneys (95% in 1 h). Radio-HPLC analysis of plasma and urine samples showed a stable radiotracer at least up to 60 min post-injection. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 03624803
- Volume :
- 56
- Issue :
- 5
- Database :
- Complementary Index
- Journal :
- Journal of Labelled Compounds & Radiopharmaceuticals
- Publication Type :
- Academic Journal
- Accession number :
- 87564439
- Full Text :
- https://doi.org/10.1002/jlcr.3016