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

Abstract : 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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https://hal-normandie-univ.archives-ouvertes.fr/hal-02466870
Contributor : Madeleine Roux-Merlin <>
Submitted on : Tuesday, February 4, 2020 - 4:34:00 PM
Last modification on : Thursday, July 2, 2020 - 3:19:25 AM

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Victor Babin, Benjamin 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, Elsevier, 2020, 96, pp.103582. ⟨10.1016/j.bioorg.2020.103582⟩. ⟨hal-02466870⟩

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