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Title: Combining rimonabant and fentanyl in a single entity: preparation and pharmacological results.
Authors: Fernández-Fernández, Cristina
Callado, Luis F
Girón, Rocío
Sánchez, Eva
Erdozain, Amaia M
López-Moreno, José Antonio
Morales, Paula
Rodríguez de Fonseca, Fernando
Fernández-Ruiz, Javier
Goya, Pilar
Meana, J Javier
Martín, M Isabel
Jagerovic, Nadine
metadata.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.
Keywords: Fentanyl;Rimonabant;Cannabinoid;Opioid;Behavioral assays;Autopsia;Cannabinoides;Opioides;moduladores de los receptores de cannabinoides;Encéfalo;Interacciones farmacológicas
metadata.dc.subject.mesh: Medical Subject Headings::Chemicals and Drugs::Heterocyclic Compounds::Heterocyclic Compounds, 1-Ring::Piperidines::Fentanyl
Medical Subject Headings::Chemicals and Drugs::Organic Chemicals::Hydrocarbons::Terpenes::Cannabinoids
Medical Subject Headings::Chemicals and Drugs::Chemical Actions and Uses::Pharmacologic Actions::Physiological Effects of Drugs::Central Nervous System Depressants::Narcotics
Medical Subject Headings::Analytical, Diagnostic and Therapeutic Techniques and Equipment::Investigative Techniques::Autopsy
Medical Subject Headings::Anatomy::Nervous System::Central Nervous System::Brain
Medical Subject Headings::Phenomena and Processes::Physiological Phenomena::Pharmacological Phenomena::Pharmacological Processes::Drug Interactions
Medical Subject Headings::Chemicals and Drugs::Chemical Actions and Uses::Pharmacologic Actions::Molecular Mechanisms of Pharmacological Action::Neurotransmitter Agents::Cannabinoid Receptor Modulators
Issue Date: 20-Feb-2014
Citation: Fernández-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; 8:263-77
Abstract: Based 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.
Description: Journal Article; Research Support, Non-U.S. Gov't;
metadata.dc.identifier.doi: 10.2147/DDDT.S55045
ISSN: 1177-8881 (Online)
Appears in Collections:01- Artículos - Hospital Regional de Málaga
01- Artículos - IBIMA. Instituto de Investigación Biomédica de Málaga

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