1245896-12-1Relevant articles and documents
Radioiododestannyllation of novel GHB neuroreceptor ligands
Pedersen, Martin,Hog, Signe,Wellendorph, Petrine,Martiny, Lars
, p. 318 - 320 (2010)
A series of 4-substituted gamma-hydroxybutyric acid (GHB) analogues have previously been synthesized and characterized for binding to specific high-affinity GHB sites in rat brain cortical membranes.1,2 Within this series some halogenated analogues displayed unprecedented high affinity and selectivity for GHB sites, and would potentially be valuable as pharmacological tools if radiolabelled. Here we present the iodine-125 labelling of one of these analogues by radioiodo-destannylation. Copyright
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
Sabbatini, Paola,Wellendorph, Petrine,H?g, Signe,Pedersen, Martin H. F.,Br?uner-Osborne, Hans,Martiny, Lars,Fr?lund, Bente,Clausen, Rasmus P.
experimental part, p. 6506 - 6510 (2010/11/18)
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.