RT Journal Article
T1 Combining rimonabant and fentanyl in a single entity: preparation and pharmacological results.
A1 Fernández-Fernández, Cristina
A1 Callado, Luis F
A1 Girón, Rocío
A1 Sánchez, Eva
A1 Erdozain, Amaia M
A1 López-Moreno, José Antonio
A1 Morales, Paula
A1 Rodríguez de Fonseca, Fernando
A1 Fernández-Ruiz, Javier
A1 Goya, Pilar
A1 Meana, J Javier
A1 Martín, M Isabel
A1 Jagerovic, Nadine
K1 Fentanyl
K1 Rimonabant
K1 Cannabinoid
K1 Opioid
K1 Behavioral assays
K1 Autopsia
K1 Cannabinoides
K1 Opioides
K1 moduladores de los receptores de cannabinoides
K1 Encéfalo
K1 Interacciones farmacológicas
AB 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.
SN 1177-8881 (Online)
YR 2014
FD 2014-02-20
LK http://hdl.handle.net/10668/1607
UL http://hdl.handle.net/10668/1607
LA en
NO 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
NO Journal Article; Research Support, Non-U.S. Gov't;
DS RISalud
RD Apr 14, 2025