Development of Molecular Probes for the Human 5-HT6 Receptor

详细信息    查看全文

• 作者：Henar Vzquez-Villa ; Juan A. Gonzlez-Vera ; Bellinda Benham ; Alma Viso ; Roberto Fernndez de la Pradilla ; Elena Junquera ; Emilio Aicart ; Mara L. Lpez-Rodrguez ; Silvia Ortega-Gutirrez
• 刊名：Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：October 14, 2010
• 年：2010
• 卷：53
• 期：19
• 页码：7095-7106
• 全文大小：1079K
• 年卷期：v.53,no.19(October 14, 2010)
• ISSN：1520-4804

文摘

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 (K_i = 175 nM and Φ_f = 0.21) and biotinylated derivative 15 (K_i = 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.