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Selective Nonpeptidic Fluorescent Ligands for Oxytocin Receptor: Design, Synthesis, and Application to Time-Resolved FRET Binding Assay

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Laboratoire d’Innovation Thérapeutique, UMR7200 CNRS/Université de Strasbourg, Labex MEDALIS, Faculté de Pharmacie, 74 route du Rhin, 67401 Illkirch, France
Institut de Génomique Fonctionnelle, Département de Pharmacologie Moléculaire, CNRS UMR 5203, INSERM U1191, Université de Montpellier, 141 rue de la Cardonille, 34094 Montpellier Cedex 5, France
§ Cisbio Bioassays, Parc Marcel Boiteux, 30200 Codolet, France
*For T.D.: phone, +33 434 35 92 64; E-mail, [email protected]
*For D.B.: phone, +33 368 85 42 36; E-mail, [email protected]
Cite this: J. Med. Chem. 2015, 58, 5, 2547–2552
Publication Date (Web):February 2, 2015
Copyright © 2015 American Chemical Society

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    Abstract Image

    The design and the synthesis of the first high-affinity fluorescent ligands for oxytocin receptor (OTR) are described. These compounds enabled the development of a TR-FRET based assay for OTR, readily amenable to high throughput screening. The validation of the assay was achieved by competition experiments with both peptide and nonpeptide OTR ligands as competitors. These probes represent the first selective fluorescent ligands for the oxytocin G protein-coupled receptor.

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    Synthesis and full characterization of compounds 59 and 1114; functional characterization of the SNAP-tag labeled OTR. This material is available free of charge via the Internet at

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