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oai:docta.ucm.es:20.500.14352/1145282025-01-16T01:08:56Zcom_20.500.14352_14col_20.500.14352_15

Vázquez Villa, María Del Henar González Vera, Juan Antonio Benhamú Salama, Bellinda Viso, Alma Fernandez de la Pradilla, Roberto Junquera González, María Elena Aicart Sospedra, Emilio López Rodríguez, María Luz Ortega Gutiérrez, Silvia 2025-01-15T17:29:03Z 2025-01-15T17:29:03Z 2010-10-14 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 0022-2623 10.1021/jm1007177 https://hdl.handle.net/20.500.14352/114528 1520-4804 https://doi.org/10.1021/jm1007177 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. eng http://creativecommons.org/licenses/by-nc-nd/4.0/ restricted access Attribution-NonCommercial-NoDerivatives 4.0 International Development of molecular probes for the human 5-HT6 receptor journal article