Design of iodinated radioligands for SPECT imaging of central human 5-HT4R using a ligand lipophilicity efficiency approach - Normandie Université Accéder directement au contenu
Article Dans Une Revue Bioorganic Chemistry Année : 2020

Design of iodinated radioligands for SPECT imaging of central human 5-HT4R using a ligand lipophilicity efficiency approach

Résumé

A series of iodinated ligands for the SPECT imaging of 5-HT4 receptors was designed starting from the previously reported hit MR-26132. We focused on the modulation of the piperidine-containing lateral chain by introducing hydrophilic groups in order to decrease the liphophilicity of the new ligands. All the synthesized compounds were tested for their binding affinities on 5-HT4Rs and based on the Ligand Lipophilicity Efficiency approach, compound 13 was further selected for radioiodination with iodine-125 and imaging experiments. Compound 13 showed its ability to displace the specific signal of the reference compound [125I]SB-207710 but no significant detection of [125I]13 was observed in vivo in SPECT experiments.

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Chimie
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Dates et versions

hal-02466870 , version 1 (07-03-2022)

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Paternité - Pas d'utilisation commerciale

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Victor Babin, Benjamin B. Tournier, Audrey Davis, Emmanuelle Dubost, Gilbert Pigrée, et al.. Design of iodinated radioligands for SPECT imaging of central human 5-HT4R using a ligand lipophilicity efficiency approach. Bioorganic Chemistry, 2020, 96, pp.103582. ⟨10.1016/j.bioorg.2020.103582⟩. ⟨hal-02466870⟩
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