用于人类 5-HT(6)受体的分子探针的开发。
Development of molecular probes for the human 5-HT(6) receptor.
机构信息
Departamento de Química Orgánica I, Facultad de Ciencias Quı´micas, Universidad Complutense deMadrid, E-28040 Madrid, Spain.
出版信息
J Med Chem. 2010 Oct 14;53(19):7095-106. doi: 10.1021/jm1007177.
In this work we report the synthesis of a set of labeled ligands targeting the human 5-HT(6) receptor (h5-HT(6)R). 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-HT(6)R in cells. Thus, they represent the first molecular probes for 5-HT(6)R visualization. These results are the starting point for introducing a variety of tags in these or other 5-HT(6)R ligand scaffolds aimed at the development of optimized probes with tailored profiles in terms of fluorescence, affinity, or selectivity.
在这项工作中，我们报告了一组针对人 5-羟色胺 6 受体 (h5-HT6R) 的标记配体的合成。在所合成的化合物中，荧光探针 10（K(i) = 175 nM 和 Φ(f) = 0.21）和生物素化衍生物 15（K(i) = 90 nM）值得特别关注，因为它们能够直接观察细胞中的 h5-HT6R。因此，它们代表了用于 5-HT6R 可视化的第一个分子探针。这些结果为在这些或其他 5-HT6R 配体支架中引入各种标记物奠定了基础，旨在开发具有针对荧光、亲和力或选择性等方面优化的探针。
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