Vázquez Villa, María Del HenarGonzález Vera, Juan AntonioBenhamú Salama, BellindaViso, AlmaFernandez de la Pradilla, RobertoJunquera González, María ElenaAicart Sospedra, EmilioLópez Rodríguez, María LuzOrtega Gutiérrez, Silvia2025-01-152025-01-152010-10-14Vázquez-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), 7095-71060022-262310.1021/jm1007177https://hdl.handle.net/20.500.14352/114528In 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.engAttribution-NonCommercial-NoDerivatives 4.0 Internationalhttp://creativecommons.org/licenses/by-nc-nd/4.0/journal article1520-4804https://doi.org/10.1021/jm1007177restricted access547Serotonin 5-HT6 receptorGPCRMolecular probesReceptor visualizationQuímica orgánica (Química)2306 Química Orgánica2390.01 Diseño. Síntesis y Estudio Nuevos Fármacos