RT Journal Article
T1 Development of molecular probes for the human 5-HT6 receptor
A1 Vázquez Villa, María Del Henar
A1 González Vera, Juan Antonio
A1 Benhamú Salama, Bellinda
A1 Viso, Alma
A1 Fernandez de la Pradilla, Roberto
A1 Junquera González, María Elena
A1 Aicart Sospedra, Emilio
A1 López Rodríguez, María Luz
A1 Ortega Gutiérrez, Silvia
AB 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.
PB ACS Publications
SN 0022-2623
YR 2010
FD 2010-10-14
LK https://hdl.handle.net/20.500.14352/114528
UL https://hdl.handle.net/20.500.14352/114528
LA eng
NO 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
NO Ministerio de Ciencia e Innovación
NO Comunidad de Madrid
DS Docta Complutense
RD 22 abr 2025