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Combining rimonabant and fentanyl in a single entity: preparation and pharmacological results.

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dc.contributor.authorFernández-Fernández, Cristina
dc.contributor.authorCallado, Luis F
dc.contributor.authorGirón, Rocío
dc.contributor.authorSánchez, Eva
dc.contributor.authorErdozain, Amaia M
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, J Javier
dc.contributor.authorMartín, M Isabel
dc.contributor.authorJagerovic, Nadine
dc.contributor.authoraffiliation[Fernández-Fernández,C; Morales,P; Goya,P; Jagerovic,N] Instituto de Química Médica, CSIC, Madrid. [Callado,LF; Erdozain,AM; Meana,JJ] Departamento de Farmacología, Universidad del Pais Vasco, UPV/EHU, CIBERSAM, Leioa. [Girón,R; Sánchez,E; Martín,MI] Departamento de Farmacología y Nutrición, Ciencias de la Salud, Universidad Rey Juan Carlos, Alcorcón. [López-Moreno,JA] Departamento de Psicobiologia, Universidad Complutense de Madrid, Madrid. [Rodríguez de Fonseca,F] Laboratorio de Medicina Regenerativa, Hospital Carlos Haya, Fundación IMABIS, Málaga. [Fernández-Ruiz,J] Departamento de Bioquímica y Biología Molecular, Facultad de Medicina, CIBERNED, IRYCIS, Universidad Complutense de Madrid, Madrid, Spain.es
dc.contributor.funderThis 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 Gov¬ernment (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 Investigación Biomédica 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 Ampliación de Estudios, cofinanced by the European Social Fund.
dc.date.accessioned2014-05-21T07:50:00Z
dc.date.available2014-05-21T07:50:00Z
dc.date.issued2014-02-20
dc.descriptionJournal Article; Research Support, Non-U.S. Gov't;es
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 wellknown drugs, ie, rimonabant and fentanyl. The new compounds have been tested for their affinity and functionality regarding CB1 and CB2 cannabinoid and μ opioid receptors. In [(35)S]-GTPγS (guanosine 5'-O-[gamma-thio]triphosphate) binding assays from the post-mortem human frontal cortex, they proved to be CB1 cannabinoid antagonists and μ opioid antagonists. Interestingly, in vivo, the new compounds exhibited a significant dual antagonist action on the endocannabinoid and opioid systems.es
dc.description.versionYeses
dc.identifier.citationFernández-Fernández C, Callado LF, Girón R, Sánchez E, Erdozain AM, López-Moreno JA, et al. Combining rimonabant and fentanyl in a single entity: preparation and pharmacological results. Drug Des Devel Ther. 2014; 8:263-77es
dc.identifier.doi10.2147/DDDT.S55045
dc.identifier.issn1177-8881 (Online)
dc.identifier.pmcPMC3934591
dc.identifier.pmid24591816
dc.identifier.urihttp://hdl.handle.net/10668/1607
dc.journal.titleDrug design, development and therapy
dc.language.isoen
dc.relation.publisherversionhttp://www.dovepress.com/combining-rimonabant-and-fentanyl-in-a-single-entity-preparation-and-p-peer-reviewed-article-DDDTes
dc.rights.accessRightsopen access
dc.subjectFentanyles
dc.subjectRimonabantes
dc.subjectCannabinoides
dc.subjectOpioides
dc.subjectBehavioral assayses
dc.subjectAutopsiaes
dc.subjectCannabinoideses
dc.subjectOpioideses
dc.subjectmoduladores de los receptores de cannabinoideses
dc.subjectEncéfaloes
dc.subjectInteracciones farmacológicases
dc.subject.meshMedical Subject Headings::Chemicals and Drugs::Heterocyclic Compounds::Heterocyclic Compounds, 1-Ring::Piperidines::Fentanyles
dc.subject.meshMedical Subject Headings::Chemicals and Drugs::Organic Chemicals::Hydrocarbons::Terpenes::Cannabinoidses
dc.subject.meshMedical Subject Headings::Chemicals and Drugs::Chemical Actions and Uses::Pharmacologic Actions::Physiological Effects of Drugs::Central Nervous System Depressants::Narcoticses
dc.subject.meshMedical Subject Headings::Analytical, Diagnostic and Therapeutic Techniques and Equipment::Investigative Techniques::Autopsyes
dc.subject.meshMedical Subject Headings::Anatomy::Nervous System::Central Nervous System::Braines
dc.subject.meshMedical Subject Headings::Phenomena and Processes::Physiological Phenomena::Pharmacological Phenomena::Pharmacological Processes::Drug Interactionses
dc.subject.meshMedical Subject Headings::Chemicals and Drugs::Chemical Actions and Uses::Pharmacologic Actions::Molecular Mechanisms of Pharmacological Action::Neurotransmitter Agents::Cannabinoid Receptor Modulatorses
dc.titleCombining rimonabant and fentanyl in a single entity: preparation and pharmacological results.es
dc.typeresearch article
dc.type.hasVersionVoR
dspace.entity.typePublication

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