Radiolabeling of [11C]FPS-ZM1, a receptor for advanced glycation end products-targeting positron emission tomography radiotracer, using a [11C]CO2-to-[11C]CO chemical conversion / Federico Luzi, Vilius Savickas, Carlotta Taddei, Stefan Hader, Nisha Singh, Antony D Gee, Salvatore Bongarzone
Aim:The receptor for advanced glycation end products (RAGE) is a viable target for early Alzheimer’s disease (AD) diagnosis using positron emission tomography (PET) as RAGE overexpression precedes Aβ plaque formation. The development of a carbon-11 analog of FPS-ZM1 (N-benzyl-4-chloro-N-cyclohexylbenzamide, [11C]FPS-ZM1), possessing nanomolar affinity for RAGE, may enable the imaging of RAGE for early AD detection.Methodology & results:Herein we report an optimized [11C]CO2-to-[11C]CO chemical conversion for the synthesis of [11C]FPS-ZM1 andin vitrobrain autoradiography. The [11C]CO2-to-[11C]CO conversion via11C-silanecarboxylate derivatives was achieved with a 57% yield within 30 s from end of [11C]CO2delivery. [11C]FPS-ZM1 was obtained with a decay-corrected isolated radiochemical yield of 9.5%.Conclusion:[11C]FPS-ZM1 distribution in brain tissues of wild-type versus transgenic AD model mice showed no statistically significant difference and high nondisplaceable binding. Aim: 11 Methodology & results: 11 2 11 11 in vitro 11 2 11 11 11 2 11 Conclusion: 11.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:12 |
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| Enthalten in: |
Future medicinal chemistry - 12(2020), 6, Seite 511- |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Luzi, Federico [VerfasserIn] |
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| Links: |
FID Access [lizenzpflichtig] |
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| Umfang: |
1 Online-Ressource (11 p) |
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| doi: |
10.4155/fmc-2019-0329 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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KFL001071424 |
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| 245 | 1 | 0 | |a Radiolabeling of [11C]FPS-ZM1, a receptor for advanced glycation end products-targeting positron emission tomography radiotracer, using a [11C]CO2-to-[11C]CO chemical conversion |c Federico Luzi, Vilius Savickas, Carlotta Taddei, Stefan Hader, Nisha Singh, Antony D Gee, Salvatore Bongarzone |
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| 520 | |a Aim:The receptor for advanced glycation end products (RAGE) is a viable target for early Alzheimer’s disease (AD) diagnosis using positron emission tomography (PET) as RAGE overexpression precedes Aβ plaque formation. The development of a carbon-11 analog of FPS-ZM1 (N-benzyl-4-chloro-N-cyclohexylbenzamide, [11C]FPS-ZM1), possessing nanomolar affinity for RAGE, may enable the imaging of RAGE for early AD detection.Methodology & results:Herein we report an optimized [11C]CO2-to-[11C]CO chemical conversion for the synthesis of [11C]FPS-ZM1 andin vitrobrain autoradiography. The [11C]CO2-to-[11C]CO conversion via11C-silanecarboxylate derivatives was achieved with a 57% yield within 30 s from end of [11C]CO2delivery. [11C]FPS-ZM1 was obtained with a decay-corrected isolated radiochemical yield of 9.5%.Conclusion:[11C]FPS-ZM1 distribution in brain tissues of wild-type versus transgenic AD model mice showed no statistically significant difference and high nondisplaceable binding. Aim: 11 Methodology & results: 11 2 11 11 in vitro 11 2 11 11 11 2 11 Conclusion: 11 | ||
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| 700 | 1 | |a Gee, Antony D |e verfasserin |4 aut | |
| 700 | 1 | |a Bongarzone, Salvatore |e verfasserin |4 aut | |
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