Por favor, use este identificador para citar o enlazar este Item:http://hdl.handle.net/20.500.12105/17058
Título
Combining rimonabant and fentanyl in a single entity: preparation and pharmacological results.
Autor(es)
Fecha de publicación
2014-02-20
Idioma
Inglés
Tipo de documento
research article
Resumen
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.
Palabras clave
Fentanyl | Rimonabant | Cannabinoid | Opioid | Behavioral assays | Autopsia | Cannabinoides | Opioides | moduladores de los receptores de cannabinoides | Encéfalo | Interacciones farmacológicas
MESH
Fentanyl | Cannabinoids | Narcotics | Autopsy | Brain | Drug Interactions | Cannabinoid Receptor Modulators
Versión en línea
DOI
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