%0 Journal Article
%A Medina, Rocio A.
%A Vázquez Villa, María Del Henar
%A Gómez Tamayo, José C.
%A Benhamú Salama, Bellinda
%A Martín-Fontecha Corrales, María Del Mar
%A de la Fuente, Tania
%A Caltabiano, Gianluigi
%A Hedlund, Peter B.
%A Pardo, Leonardo
%A López Rodríguez, María Luz
%T The extracellular entrance provides selectivity to serotonin 5-HT7 receptor antagonists with antidepressant-like behavior in vivo
%D 2014
%@ 0022-2623
%U https://hdl.handle.net/20.500.14352/114419
%X 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.
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