The extracellular entrance provides selectivity to serotonin 5-HT <inf>7</inf> receptor antagonists with antidepressant-like behavior in vivo

Rocío A. Medina, Henar Vázquez-Villa, José C. Gómez-Tamayo, Bellinda Benhamú, Mar Martín-Fontecha, Tania De La Fuente, Gianluigi Caltabiano, Peter B. Hedlund, Leonardo Pardo, María L. López-Rodríguez

Research output: Contribution to journalArticleResearchpeer-review

10 Citations (Scopus)

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. © 2014 American Chemical Society.
Original languageEnglish
Pages (from-to)6879-6884
JournalJournal of Medicinal Chemistry
Volume57
Issue number15
DOIs
Publication statusPublished - 14 Aug 2014

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