RT Journal Article
T1 Development of fluorescent ligands for the human 5-HT1A receptor
A1 Alonso, Dulce
A1 Vázquez Villa, María Del Henar
A1 Gamo, Ana M.
A1 Martínez Esperón, Maria F.
A1 Tortosa, Mariola
A1 Viso, Alma
A1 Fernández de la Pradilla, Roberto
A1 Junquera González, María Elena
A1 Aicart Sospedra, Emilio
A1 Martín-Fontecha Corrales, María Del Mar
A1 Benhamú Salama, Bellinda
A1 López Rodríguez, María Luz
A1 Ortega Gutiérrez, Silvia
AB In this work, we report the design and synthesis of a set of fluorescent probes targeting the human 5-HT1A receptor (h5-HT1AR). Among the synthesized compounds, derivative 4 deserves special attention as being a high-affinity ligand (Ki = 2 nM) with good fluorescent properties (Iem > 1000 au and a fluorescence quantum yield, Φf, of 0.26), which enables direct observation of the h5-HT1AR in cells. Thus, it represents the first efficacious fluorescent probe for the specific labeling of h5-HT1AR in cells. Our results provide the basis for the introduction of a variety of tags in scaffolds of G protein-coupled receptor (GPCR) ligands that enable visualization, covalent binding, or affinity pull-down of receptors. These strategies should contribute to the optimization of the therapeutic exploitation of known or new members of the GPCR superfamily by providing valuable information about their location or level of expression.
PB ACS Publications
SN 1948-5875
YR 2010
FD 2010-09-01
LK https://hdl.handle.net/20.500.14352/114435
UL https://hdl.handle.net/20.500.14352/114435
LA eng
NO Alonso, D., Vázquez-Villa, H.,  Gamo, A. M., Martínez-Esperón, M. F., Tortosa, M., Viso, A., de la Pradilla, R.F., Junquera, E., Aicart, E. ; Martín-Fontecha, M., Benhamú, B.,  López-Rodríguez, M. L., Ortega-Gutiérrez, S. Development of Fluorescent Ligands for the Human 5-HT1A Receptor. ACS Med. Chem. Lett. 2010, 1 (6), 249-253
NO Ministerio de Ciencia, Innovación y Universidades
NO Comunidad de Madrid
DS Docta Complutense
RD 11 abr 2025