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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.
dc.date.accessioned2024-01-15T18:17:06Z
dc.date.available2024-01-15T18:17:06Z
dc.date.issued2014-02-20
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.
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 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.identifier.doi10.2147/DDDT.S55045
dc.identifier.issn1177-8881
dc.identifier.journalDrug design, development and therapyes_ES
dc.identifier.otherhttp://hdl.handle.net/10668/1607
dc.identifier.pubmedID24591816es_ES
dc.identifier.urihttp://hdl.handle.net/20.500.12105/17058
dc.language.isoeng
dc.relation.publisherversionhttp://www.dovepress.com/combining-rimonabant-and-fentanyl-in-a-single-entity-preparation-and-p-peer-reviewed-article-DDDTes
dc.rights.accessRightsopen accesses_ES
dc.rights.licenseAttribution-NonCommercial 4.0 International*
dc.rights.urihttps://creativecommons.org/licenses/by-nc/4.0/*
dc.subjectFentanyl
dc.subjectRimonabant
dc.subjectCannabinoid
dc.subjectOpioid
dc.subjectBehavioral assays
dc.subjectAutopsia
dc.subjectCannabinoides
dc.subjectOpioides
dc.subjectmoduladores de los receptores de cannabinoides
dc.subjectEncéfalo
dc.subjectInteracciones farmacológicas
dc.subject.meshFentanyl
dc.subject.meshCannabinoids
dc.subject.meshNarcotics
dc.subject.meshAutopsy
dc.subject.meshBrain
dc.subject.meshDrug Interactions
dc.subject.meshCannabinoid Receptor Modulators
dc.titleCombining rimonabant and fentanyl in a single entity: preparation and pharmacological results.
dc.typeresearch article
dc.type.hasVersionVoR
dspace.entity.typePublication

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IBIMA-Plataforma BIONAND - Instituto de Investigación Biomédica de Málaga y Plataforma en Nanomedicina (Andalucía)
IRYCIS - Instituto Ramón y Cajal de Investigación Sanitaria (Madrid)