%0 Journal Article
%A Vázquez Villa, María Del Henar
%A González Vera, Juan Antonio
%A Benhamú Salama, Bellinda
%A Viso, Alma
%A Fernandez de la Pradilla, Roberto
%A Junquera González, María Elena
%A Aicart Sospedra, Emilio
%A López Rodríguez, María Luz
%A Ortega Gutiérrez, Silvia
%T Development of molecular probes for the human 5-HT6 receptor
%D 2010
%@ 0022-2623
%U https://hdl.handle.net/20.500.14352/114528
%X 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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