Microfluidic radiosynthesis of [18F]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...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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Beilstein-Institut
2017-12-01
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| Series: | Beilstein Journal of Organic Chemistry |
| Subjects: | |
| Online Access: | https://doi.org/10.3762/bjoc.13.285 |
| _version_ | 1818657384688517120 |
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| author | Thomas Lee Collier Steven H. Liang J. John Mann Neil Vasdev J. S. Dileep Kumar |
| author_facet | Thomas Lee Collier Steven H. Liang J. John Mann Neil Vasdev J. S. Dileep Kumar |
| author_sort | Thomas Lee Collier |
| collection | DOAJ |
| 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 18F-labeling. In this paper, we report on the two-step microfluidic radiosynthesis of the high affinity partial agonist of the serotonin 1A receptor, [18F]FEMPT (pKi = 9. 79; Ki = 0.16 nM) by microfluidic radiochemistry. [18F]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). |
| first_indexed | 2024-12-17T03:40:38Z |
| format | Article |
| id | doaj.art-f2d3b8f0f0bc4f6984684e32c5bebcdd |
| institution | Directory Open Access Journal |
| issn | 1860-5397 |
| language | English |
| last_indexed | 2024-12-17T03:40:38Z |
| publishDate | 2017-12-01 |
| publisher | Beilstein-Institut |
| record_format | Article |
| series | Beilstein Journal of Organic Chemistry |
| spelling | doaj.art-f2d3b8f0f0bc4f6984684e32c5bebcdd2022-12-21T22:05:01ZengBeilstein-InstitutBeilstein Journal of Organic Chemistry1860-53972017-12-011312922292710.3762/bjoc.13.2851860-5397-13-285Microfluidic radiosynthesis of [18F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptorsThomas Lee Collier0Steven H. Liang1J. John Mann2Neil Vasdev3J. S. Dileep Kumar4Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Harvard Medical School, Boston, MA, USADivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Harvard Medical School, Boston, MA, USAMolecular Imaging and Neuropathology Division, New York State Psychiatric Institute, New York, NY, USAAdvion, Inc., Ithaca, NY, USAMolecular Imaging and Neuropathology Division, New York State Psychiatric Institute, New York, NY, USAContinuous-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 18F-labeling. In this paper, we report on the two-step microfluidic radiosynthesis of the high affinity partial agonist of the serotonin 1A receptor, [18F]FEMPT (pKi = 9. 79; Ki = 0.16 nM) by microfluidic radiochemistry. [18F]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).https://doi.org/10.3762/bjoc.13.285agonistfluorine-185-HT1AmicrofluidicsPET |
| spellingShingle | Thomas Lee Collier Steven H. Liang J. John Mann Neil Vasdev J. S. Dileep Kumar Microfluidic radiosynthesis of [18F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptors Beilstein Journal of Organic Chemistry agonist fluorine-18 5-HT1A microfluidics PET |
| title | Microfluidic radiosynthesis of [18F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptors |
| title_full | Microfluidic radiosynthesis of [18F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptors |
| title_fullStr | Microfluidic radiosynthesis of [18F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptors |
| title_full_unstemmed | Microfluidic radiosynthesis of [18F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptors |
| title_short | Microfluidic radiosynthesis of [18F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptors |
| title_sort | microfluidic radiosynthesis of 18f fempt a high affinity pet radiotracer for imaging serotonin receptors |
| topic | agonist fluorine-18 5-HT1A microfluidics PET |
| url | https://doi.org/10.3762/bjoc.13.285 |
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