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Development of molecular probes for the human 5-HT6 receptor

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https://doi.org/10.1021/jm1007177

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2010

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ACS Publications
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https://hdl.handle.net/20.500.14352/114528

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Vázquez-Villa, H., González-Vera, J. A., Benhamú, B., Viso, A., Fernández de la Pradilla, R., Junquera, E., Aicart, E., López-Rodríguez, M. L., Ortega-Gutiérrez, S. Development of Molecular Probes for the Human 5-HT6 Receptor. J. Med. Chem. 2010, 53 (19), 7095-7106

Abstract

In this work we report the synthesis of a set of labeled ligands targeting the human 5-HT6 receptor (h5-HT6R). Among the synthesized compounds, fluorescent probe 10 (Ki = 175 nM and Φf = 0.21) and biotinylated derivative 15 (Ki = 90 nM) deserve special attention because they enable direct observation of the h5-HT6R in cells. Thus, they represent the first molecular probes for 5-HT6R visualization. These results are the starting point for introducing a variety of tags in these or other 5-HT6R ligand scaffolds aimed at the development of optimized probes with tailored profiles in terms of fluorescence, affinity, or selectivity.

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Química orgánica (Química)

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2306 Química Orgánica, 2390.01 Diseño. Síntesis y Estudio Nuevos Fármacos

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