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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...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Beilstein-Institut
2017
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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). |
format | Online Article Text |
id | pubmed-5753126 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | Beilstein-Institut |
record_format | MEDLINE/PubMed |
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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