Design, Synthesis, and in Vitro Pharmacology of New Radiolabeled γ-Hydroxybutyric Acid Analogues Including Photolabile Analogues with Irreversible Binding to the High-Affinity γ-Hydroxybutyric Acid Binding Sites

Paola Sabbatini, Petrine Wellendorph, Signe Høg, Martin Holst Friborg Pedersen, Hans Bruner-Osborne, Lars Martiny, Bente Frølund, Rasmus P. Clausen

    Research output: Contribution to journalJournal articleResearchpeer-review

    Abstract

    γ-Hydroxybutyric acid (GHB) is a psychotropic compound endogenous to the brain. Despite its potential physiological significance, the complete molecular mechanisms of action remain unexplained. To facilitate the isolation and identification of the high-affinity GHB binding site, we herein report the design and synthesis of the first 125I-labeled radioligands in the field, one of which contains a photoaffinity label which enables it to bind irreversibly to the high-affinity GHB binding sites.
    Original languageEnglish
    JournalJournal of Medicinal Chemistry
    Volume53
    Issue number17
    Pages (from-to)6506-6510
    ISSN0022-2623
    DOIs
    Publication statusPublished - 2010

    Keywords

    • Hevesy laboratory
    • Radiation research and nuclear technologies

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