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Synthèse de ligands iodés et fluorés en série indazole : application en imagerie des récepteurs 5-HT4 centraux

Abstract : Since their discovery in 1989, type 4 serotonin receptors (5-HT4R) have become a target of choice in the development of new diagnostic and therapeutic tools. Indeed, their involvement in neuropsychiatric disorders such as depression or anorexia and in neurodegenerative diseases such as Alzheimer's disease (AD) have motivated many research teams to characterize them via the development of radiotracers that are potent and specific toward this target.Currently, none of them can be used in humans, limiting the prospects for early diagnosis of these pathologies. Thus, we decided to develop a new series of ligands with affinity toward 5-HT4R on the fluoroindazole series with the final objective to develop a new radiotracer that can be used in PET imaging (Positron Emission Tomodensitometry). We have established a new convergent and efficient synthetic pathway allowing us to access, in a minimum of steps, more than twenty new ligands with nanomolar affinity for 5-HT4R. Among them, we selected three compounds of interest as "lead" for radiolabelling with fluorine-18. This selection is the result of a multiparametric approach highlighting the remarkable properties of the best compounds.Currently, MR35806 is in the process for radiolabelling, giving us hope of obtaining the first potent and selective 5-HT4R radiotracer for PET imaging.
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Submitted on : Saturday, June 19, 2021 - 1:01:47 AM
Last modification on : Wednesday, November 3, 2021 - 7:20:24 AM
Long-term archiving on: : Monday, September 20, 2021 - 6:06:02 PM


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  • HAL Id : tel-03265143, version 1


Reynald Mangeant. Synthèse de ligands iodés et fluorés en série indazole : application en imagerie des récepteurs 5-HT4 centraux. Médecine humaine et pathologie. Normandie Université, 2020. Français. ⟨NNT : 2020NORMC419⟩. ⟨tel-03265143⟩



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