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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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dc.contributor.authorMedina, Rocio A.
dc.contributor.authorVázquez Villa, María Del Henar
dc.contributor.authorGómez Tamayo, José C.
dc.contributor.authorBenhamú Salama, Bellinda
dc.contributor.authorMartín-Fontecha Corrales, María Del Mar
dc.contributor.authorde la Fuente, Tania
dc.contributor.authorCaltabiano, Gianluigi
dc.contributor.authorHedlund, Peter B.
dc.contributor.authorPardo, Leonardo
dc.contributor.authorLópez Rodríguez, María Luz
dc.date.accessioned2025-01-15T11:28:19Z
dc.date.available2025-01-15T11:28:19Z
dc.date.issued2014-08-14
dc.description.abstractThe 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.
dc.description.departmentDepto. de Química Orgánica
dc.description.facultyFac. de Ciencias Químicas
dc.description.refereedTRUE
dc.description.sponsorshipMinistería de Economía y Competetividad
dc.description.sponsorshipComunidad de Madrid
dc.description.sponsorshipFundación Ramón Areces
dc.description.statuspub
dc.identifier.citationMedina, 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
dc.identifier.doi10.1021/jm500880c
dc.identifier.essn1520-4804
dc.identifier.issn0022-2623
dc.identifier.officialurlhttps://doi.org/10.1021/jm500880c
dc.identifier.relatedurlhttps://pubs.acs.org/doi/10.1021/jm500880c
dc.identifier.urihttps://hdl.handle.net/20.500.14352/114419
dc.issue.number15
dc.journal.titleJournal of Medicinal Chemistry
dc.language.isoeng
dc.page.final6884
dc.page.initial6879
dc.publisherACS Publications
dc.relation.projectIDSAF2010-22198-C02
dc.relation.projectIDinfo:eu-repo/grantAgreement/MINECO//SAF2013-48271-C2-1-R/ES/NUEVAS DIANAS Y ESTRATEGIAS TERAPEUTICAS/
dc.relation.projectIDS2010/BMD2353
dc.rightsAttribution-NonCommercial-NoDerivatives 4.0 Internationalen
dc.rights.accessRightsrestricted access
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/
dc.subject.cdu547
dc.subject.keywordGPCR
dc.subject.keywordSerotonin 5-HT7 receptor
dc.subject.keywordSelective antagonists
dc.subject.keywordMajor depression
dc.subject.keywordAntidepressant-like effect
dc.subject.ucmQuímica orgánica (Química)
dc.subject.ucmQuímica farmaceútica
dc.subject.unesco2306 Química Orgánica
dc.subject.unesco2390.01 Diseño. Síntesis y Estudio Nuevos Fármacos
dc.titleThe extracellular entrance provides selectivity to serotonin 5-HT7 receptor antagonists with antidepressant-like behavior in vivo
dc.typejournal article
dc.type.hasVersionVoR
dc.volume.number57
dspace.entity.typePublication
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relation.isAuthorOfPublication4e4d691c-4c40-4927-8569-2109d72ab618
relation.isAuthorOfPublicationc92ce05e-a89c-46f4-a541-a45f20dc57e5
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relation.isAuthorOfPublication.latestForDiscoveryc6cf4ab4-c279-4f4a-a50e-ec9277e3798d

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