1246948-55-9Relevant academic research and scientific papers
Development of molecular probes for the human 5-HT6 receptor
Vázquez-Villa, Henar,González-Vera, Juan A.,Benhamú, Bellinda,Viso, Alma,Fernández De La Pradilla, Roberto,Junquera, Elena,Aicart, Emilio,López-Rodríguez, María L.,Ortega-Gutiérrez, Silvia
supporting information; experimental part, p. 7095 - 7106 (2010/12/25)
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 -f = 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.
