RT Journal Article
T1 The extracellular entrance provides selectivity to serotonin 5-HT7 receptor antagonists with antidepressant-like behavior in vivo
A1 Medina, Rocio A.
A1 Vázquez Villa, María Del Henar
A1 Gómez Tamayo, José C.
A1 Benhamú Salama, Bellinda
A1 Martín-Fontecha Corrales, María Del Mar
A1 de la Fuente, Tania
A1 Caltabiano, Gianluigi
A1 Hedlund, Peter B.
A1 Pardo, Leonardo
A1 López Rodríguez, María Luz
AB The finding that ergotamine binds serotonin receptors in a less conserved extended binding pocket close to the extracellular entrance, in addition to the orthosteric site, allowed us to obtain 5-HT7R antagonist 6 endowed with high affinity (Ki = 0.7 nM) and significant 5-HT1AR selectivity (ratio >1428). Compound 6 exhibits in vivo antidepressant-like effect (1 mg/kg, ip) mediated by the 5-HT7R, which reveals its interest as a putative research tool or pharmaceutical in depression disorders.
PB ACS Publications
SN 0022-2623
YR 2014
FD 2014-08-14
LK https://hdl.handle.net/20.500.14352/114419
UL https://hdl.handle.net/20.500.14352/114419
LA eng
NO Medina, R. A., Vázquez-Villa, H., Gómez-Tamayo, J. C., Benhamú, B., Martín-Fontecha, M., de la Fuente, T., Caltabiano, G., Hedlund, P. B., Pardo, L., López-Rodríguez, M. L. The Extracellular Entrance Provides Selectivity to Serotonin 5-HT7 Receptor Antagonists with Antidepressant-like Behavior in Vivo. J. Med. Chem. 2014, 57 (15), 6879-6884
NO Ministería de Economía y Competetividad
NO Comunidad de Madrid
NO Fundación Ramón Areces
DS Docta Complutense
RD 14 dic 2025