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dc.contributor.authorFernández Fernández, Cristina
dc.contributor.authorCallado Hernando, Luis Felipe ORCID
dc.contributor.authorGirón, Rocío
dc.contributor.authorSánchez, Eva
dc.contributor.authorErdozain Fernández, Amaia Maite ORCID
dc.contributor.authorLópez-Moreno, José Antonio
dc.contributor.authorMorales, Paula
dc.contributor.authorRodríguez de Fonseca, Fernando
dc.contributor.authorFernández-Ruiz, Javier
dc.contributor.authorGoya, Pilar
dc.contributor.authorMeana Martínez, José Javier ORCID
dc.contributor.authorMartín, Isabel
dc.contributor.authorJagerovic, Nadine
dc.date.accessioned2016-04-04T15:56:08Z
dc.date.available2016-04-04T15:56:08Z
dc.date.issued2014
dc.identifier.citationDrug Design, Development and Therapy 8 : 263-277(2014)es
dc.identifier.issn1177-8881
dc.identifier.urihttp://hdl.handle.net/10810/17779
dc.description.abstractBased on numerous pharmacological studies that have revealed an interaction between cannabinoid and opioid systems at the molecular, neurochemical, and behavioral levels, a new series of hybrid molecules has been prepared by coupling the molecular features of two well-known drugs, ie, rimonabant and fentanyl. The new compounds have been tested for their affinity and functionality regarding CB1 and CB2 cannabinoid and mu opioid receptors. In [S-35]-GTP.S (guanosine 5'-O-[gamma-thio] triphosphate) binding assays from the post-mortem human frontal cortex, they proved to be CB1 cannabinoid antagonists and mu opioid antagonists. Interestingly, in vivo, the new compounds exhibited a significant dual antagonist action on the endocannabinoid and opioid systems.es
dc.description.sponsorshipThis work was supported by grants from the Spanish Ministry of Economy and Competitivity (SAF2012-40075, SAF2009-12422, SAF2010-20521, SAF2011-26818), Red de Trastornos Adictivos (RETICS RD06/001), the Madrid Government (CANNAB-CM, S2010/BMD-2308), the University of the Basque Country (UFI 11/35), the Basque Government (IT-199-07, SAIOTEK S-PE10UN14), and the Instituto de Salud Carlos III, Centro de Investigacion Biomedica en Red de Salud Mental, CIBERSAM. AME is the recipient of a pre-doctoral fellowship from the Basque Government. PM is the recipient of a fellowship (JAE-Pre-2010-01119) from Junta para la Ampliacion de Estudios, cofinanced by the European Social Fund. The authors thank Laura Hernandez-Folgado for her help in preparation of the manuscript.es
dc.language.isoenges
dc.publisherDove Medical Presses
dc.rightsinfo:eu-repo/semantics/openAccesses
dc.subjectfentanyles
dc.subjectrimonabantes
dc.subjectcannabinoides
dc.subjectopioides
dc.subjectbehavioral assayses
dc.subjectpostmortem human braines
dc.subjectreceptor antagonist SR-141716es
dc.subjectI-2 imidazoline binding-siteses
dc.subjectalcohol deprivationes
dc.subjectopioid interactionses
dc.subjectfood-intakees
dc.subjectCB1es
dc.subjectratses
dc.subjectligandses
dc.subjectderivativeses
dc.titleCombining rimonabant and fentanyl in a single entity: preparation and pharmacological resultses
dc.typeinfo:eu-repo/semantics/articlees
dc.rights.holder© 2014 Fernández-Fernández et al. This work is published by Dove Medical Press Limited, and licensed under Creative Commons Attribution – Non Commercial (unported, v3.0) License. The full terms of the License are available at http://creativecommons.org/licenses/by-nc/3.0/. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. Permissions beyond the scope of the License are administered by Dove Medical Press Limited. Information on how to request permission may be found at: http://www.dovepress.com/permissions.phpes
dc.relation.publisherversionhttps://www.dovepress.com/combining-rimonabant-and-fentanyl-in-a-single-entity-preparation-and-p-peer-reviewed-article-DDDT#es
dc.identifier.doi10.2147/DDDT.S55045
dc.departamentoesFarmacologíaes_ES
dc.departamentoeuFarmakologiaes_ES
dc.subject.categoriaDRUG DISCOVERY
dc.subject.categoriaPHARMACOLOGY AND PHARMACY
dc.subject.categoriaPHARMACEUTICAL SCIENCE


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