Abstract
7-Azido-8-[ 125I]ketanserin ([ 125I]AZIK) was characterized as a potent photoaffinity probe for serotonin-S 2 receptors. In reversible binding experiments, [ 125I]AZIK bound with high affinity (K d = 0.69 nM) to rat frontal cortex membranes. When incubation with [ 125I]AZIK was followed by UV irradiation, the binding was found to be irreversible. Protection experiments with various drugs demonstrated the serotonin-S 2 nature of the photoaffinity labelling. SDS-polyacrylamide gel electrophoresis of the photolabelled membranes allowed one to identify the serotonin-S 2 receptor ligand binding site as a single polypeptide with a molecular mass of approx. 67500 Da. [ 125I]AZIK will be a valuable tool for the elucidation of the serotonin-S 2 receptor structure.
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