Fernández-Fernández, CristinaCallado, Luis FGirón, RocíoSánchez, EvaErdozain, Amaia MLópez-Moreno, José AntonioMorales, PaulaRodríguez de Fonseca, FernandoFernández-Ruiz, JavierGoya, PilarMeana, J JavierMartín, M IsabelJagerovic, Nadine2014-05-212014-05-212014-02-20Fernández-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; 8:263-771177-8881 (Online)http://hdl.handle.net/10668/1607Journal Article; Research Support, Non-U.S. Gov't;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.enFentanylRimonabantCannabinoidOpioidBehavioral assaysAutopsiaCannabinoidesOpioidesmoduladores de los receptores de cannabinoidesEncéfaloInteracciones farmacológicasMedical Subject Headings::Chemicals and Drugs::Heterocyclic Compounds::Heterocyclic Compounds, 1-Ring::Piperidines::FentanylMedical Subject Headings::Chemicals and Drugs::Organic Chemicals::Hydrocarbons::Terpenes::CannabinoidsMedical Subject Headings::Chemicals and Drugs::Chemical Actions and Uses::Pharmacologic Actions::Physiological Effects of Drugs::Central Nervous System Depressants::NarcoticsMedical Subject Headings::Analytical, Diagnostic and Therapeutic Techniques and Equipment::Investigative Techniques::AutopsyMedical Subject Headings::Anatomy::Nervous System::Central Nervous System::BrainMedical Subject Headings::Phenomena and Processes::Physiological Phenomena::Pharmacological Phenomena::Pharmacological Processes::Drug InteractionsMedical Subject Headings::Chemicals and Drugs::Chemical Actions and Uses::Pharmacologic Actions::Molecular Mechanisms of Pharmacological Action::Neurotransmitter Agents::Cannabinoid Receptor Modulatorsresearch article24591816open access10.2147/DDDT.S55045PMC3934591