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The extracellular entrance provides selectivity to serotonin 5-HT7 receptor antagonists with antidepressant-like behavior in vivo

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https://doi.org/10.1021/jm500880c

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2014

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ACS Publications
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https://hdl.handle.net/20.500.14352/114419

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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

Abstract

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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Química orgánica (Química), Química farmaceútica

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2306 Química Orgánica, 2390.01 Diseño. Síntesis y Estudio Nuevos Fármacos

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