High-affinity fluorescent ligands for the 5-HT3 receptor

Jonathan Simonin, Sanjeev Kumar V. Vernekar, Andrew J. Thompson, J. Daniel Hothersall, Christopher N. Connolly, Sarah C. R. Lummis, Martin Lochner

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    Abstract

    The synthesis, photophysical and biological characterization of a small library of fluorescent 5-HT3 receptor ligands is described. Several of these novel granisetron conjugates have high quantum yields and show high affinity for the human 5-HT(3)AR. (C) 2011 Elsevier Ltd. All rights reserved.

    Original languageEnglish
    Pages (from-to)1151-1155
    Number of pages5
    JournalBioorganic & Medicinal Chemistry Letters
    Volume22
    Issue number2
    DOIs
    Publication statusPublished - 2012

    Keywords

    • 5-HT3 receptor
    • Cys-loop ligand-gated ion channels
    • Fluorescent ligands
    • Radioligand binding
    • In vivo imaging
    • ANTAGONISTS
    • TARGET

    Cite this

    Simonin, J., Vernekar, S. K. V., Thompson, A. J., Hothersall, J. D., Connolly, C. N., Lummis, S. C. R., & Lochner, M. (2012). High-affinity fluorescent ligands for the 5-HT3 receptor. Bioorganic & Medicinal Chemistry Letters, 22(2), 1151-1155. https://doi.org/10.1016/j.bmcl.2011.11.097