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  • Title: Development of molecular probes for the human 5-HT(6) receptor.
    Author: Vázquez-Villa H, González-Vera JA, Benhamú B, Viso A, Fernández de la Pradilla R, Junquera E, Aicart E, López-Rodríguez ML, Ortega-Gutiérrez S.
    Journal: J Med Chem; 2010 Oct 14; 53(19):7095-106. PubMed ID: 20845907.
    Abstract:
    In this work we report the synthesis of a set of labeled ligands targeting the human 5-HT(6) receptor (h5-HT(6)R). Among the synthesized compounds, fluorescent probe 10 (K(i) = 175 nM and Φ(f) = 0.21) and biotinylated derivative 15 (K(i) = 90 nM) deserve special attention because they enable direct observation of the h5-HT(6)R in cells. Thus, they represent the first molecular probes for 5-HT(6)R visualization. These results are the starting point for introducing a variety of tags in these or other 5-HT(6)R ligand scaffolds aimed at the development of optimized probes with tailored profiles in terms of fluorescence, affinity, or selectivity.
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