Design, synthesis, and in vitro pharmacology of new radiolabeled ¿-hydroxybutyric acid analogues including photolabile analogues with irreversible binding to the high-affinity ¿-hydroxybutyric acid binding sites

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Paola Sabbatini, Petrine Wellendorph, Signe Høg, Martin Holst Friborg Pedersen, Hans Bräuner-Osborne, Lars Martiny, Bente Flensborg Frølund, Rasmus Prætorius Clausen

gamma-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 (125)I-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

ID: 21772547