The extracellular entrance provides selectivity to serotonin 5-HT7 receptor antagonists with antidepressant-like behavior in vivo.
Basic Information
ID: ALA3351619
Journal: J Med Chem
Title: The extracellular entrance provides selectivity to serotonin 5-HT7 receptor antagonists with antidepressant-like behavior in vivo.
Authors: Medina RA, Vázquez-Villa H, Gómez-Tamayo JC, Benhamú B, Martín-Fontecha M, de la Fuente T, Caltabiano G, Hedlund PB, Pardo L, López-Rodríguez ML.
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.
CiteXplore: 25073094
DOI: 10.1021/jm500880c
Patent ID: ┄