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Microfluidic radiosynthesis of [(18)F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptors

Continuous-flow microfluidics has shown increased applications in radiochemistry over the last decade, particularly for both pre-clinical and clinical production of fluorine-18 labeled radiotracers. The main advantages of microfluidics are the reduction in reaction times and consumption of reagents...

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Detalles Bibliográficos
Autores principales: Collier, Thomas Lee, Liang, Steven H, Mann, J John, Vasdev, Neil, Kumar, J S Dileep
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Beilstein-Institut 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5753126/
https://www.ncbi.nlm.nih.gov/pubmed/29564020
http://dx.doi.org/10.3762/bjoc.13.285
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author Collier, Thomas Lee
Liang, Steven H
Mann, J John
Vasdev, Neil
Kumar, J S Dileep
author_facet Collier, Thomas Lee
Liang, Steven H
Mann, J John
Vasdev, Neil
Kumar, J S Dileep
author_sort Collier, Thomas Lee
collection PubMed
description Continuous-flow microfluidics has shown increased applications in radiochemistry over the last decade, particularly for both pre-clinical and clinical production of fluorine-18 labeled radiotracers. The main advantages of microfluidics are the reduction in reaction times and consumption of reagents that often result in increased radiochemical yields and rapid optimization of reaction parameters for (18)F-labeling. In this paper, we report on the two-step microfluidic radiosynthesis of the high affinity partial agonist of the serotonin 1A receptor, [(18)F]FEMPT (pK(i) = 9. 79; K(i) = 0.16 nM) by microfluidic radiochemistry. [(18)F]FEMPT was obtained in ≈7% isolated radiochemical yield and in >98% radiochemical and chemical purity. The molar activity of the final product was determined to be >148 GBq/µmol (>4 Ci/µmol).
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spelling pubmed-57531262018-03-21 Microfluidic radiosynthesis of [(18)F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptors Collier, Thomas Lee Liang, Steven H Mann, J John Vasdev, Neil Kumar, J S Dileep Beilstein J Org Chem Full Research Paper Continuous-flow microfluidics has shown increased applications in radiochemistry over the last decade, particularly for both pre-clinical and clinical production of fluorine-18 labeled radiotracers. The main advantages of microfluidics are the reduction in reaction times and consumption of reagents that often result in increased radiochemical yields and rapid optimization of reaction parameters for (18)F-labeling. In this paper, we report on the two-step microfluidic radiosynthesis of the high affinity partial agonist of the serotonin 1A receptor, [(18)F]FEMPT (pK(i) = 9. 79; K(i) = 0.16 nM) by microfluidic radiochemistry. [(18)F]FEMPT was obtained in ≈7% isolated radiochemical yield and in >98% radiochemical and chemical purity. The molar activity of the final product was determined to be >148 GBq/µmol (>4 Ci/µmol). Beilstein-Institut 2017-12-29 /pmc/articles/PMC5753126/ /pubmed/29564020 http://dx.doi.org/10.3762/bjoc.13.285 Text en Copyright © 2017, Collier et al. https://creativecommons.org/licenses/by/4.0https://www.beilstein-journals.org/bjoc/termsThis is an Open Access article under the terms of the Creative Commons Attribution License (https://creativecommons.org/licenses/by/4.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. The license is subject to the Beilstein Journal of Organic Chemistry terms and conditions: (https://www.beilstein-journals.org/bjoc/terms)
spellingShingle Full Research Paper
Collier, Thomas Lee
Liang, Steven H
Mann, J John
Vasdev, Neil
Kumar, J S Dileep
Microfluidic radiosynthesis of [(18)F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptors
title Microfluidic radiosynthesis of [(18)F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptors
title_full Microfluidic radiosynthesis of [(18)F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptors
title_fullStr Microfluidic radiosynthesis of [(18)F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptors
title_full_unstemmed Microfluidic radiosynthesis of [(18)F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptors
title_short Microfluidic radiosynthesis of [(18)F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptors
title_sort microfluidic radiosynthesis of [(18)f]fempt, a high affinity pet radiotracer for imaging serotonin receptors
topic Full Research Paper
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5753126/
https://www.ncbi.nlm.nih.gov/pubmed/29564020
http://dx.doi.org/10.3762/bjoc.13.285
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