RT Journal Article
T1 Development of fluorescent probes that target serotonin 5-HT2B receptors
A1 Azuaje Guerrero, Jhonny Alberto
A1 López Martínez, Paula
A1 Iglesias Fernández, Alba
A1 Fuente, Rocío de la
A1 Pérez Rubio, José M.
A1 García Peña, Diego
A1 Stępniewski, Tomasz Maciej
A1 García Mera, Xerardo
A1 Brea Floriani, José Manuel
A1 Selent, Jana
A1 Pérez Meirás, María Dolores
A1 Castro Pérez, María de los Ángeles
A1 Loza García, María Isabel
A1 Sotelo Pérez, Eddy
AB Some 5-HT2B fluorescent probes were obtained by tagging 1-(2,5-dimethoxy-4-iodophenyl)-propan2-amine (DOI) with a subset of fluorescent amines. Some of the resulting fluorescent ligands showed excellent affinity and selectivity profiles at the 5-HT2B receptors (e.g. 12b), while retain the agonistic functional behaviour of the model ligand (DOI). The study highlighted the most salient features of the structure-activity relationship in this series and these were substantiated by a molecular modelling study based on a receptor-driven docking model constructed on the basis of the crystal structure of the human 5-HT2B receptor. One of the fluorescent ligands developed in this work, compound 12i, specifically labelled CHO-K1 cells expressing 5-HT2B receptors and not parental CHO-K1 cells in a concentration-dependent manner. 12i enables imaging and quantification of specific 5-HT2B receptor labelling in live cells by automated fluorescence microscopy as well as quantification by measurements of fluorescence intensity using a fluorescence plate reader.
PB Nature Publishing Group
YR 2017
FD 2017
LK http://hdl.handle.net/10347/22518
UL http://hdl.handle.net/10347/22518
LA eng
NO Azuaje, J., López, P., Iglesias, A. et al. Development of Fluorescent Probes that Target Serotonin 5-HT2B Receptors. Sci Rep 7, 10765 (2017). https://doi.org/10.1038/s41598-017-11370-2
NO This research was carried out within the framework of the Cost Action GLISTEN and financially supported by the Spanish Government (grant numbers SAF2009-13609-C04-03 and GPC2014/003 (PS09/63) to E.S. and SAF2014-57138-C2-1-R to M.C. and M.I.L.). Authors also thanks financial support from Consellería de Cultura, Educación e Ordenación Universitaria of the Galician Government: (grant: GPC2014/03), Centro Singular de Investigación de Galicia accreditation 2016-2019 (ED431G/09). J. S. acknowledges financial support from Instituto de Salud Carlos III FEDER (CP12/03139 and PI15/00460)
DS Minerva
RD 24 abr 2026