2026-08-29T14:05:18Zhttps://repisalud.isciii.es/rest/oai/requestoai:repisalud.isciii.es:20.500.12105/170582024-09-21T20:12:23Zcom_20.500.12105_15322com_20.500.12105_2051col_20.500.12105_16927col_20.500.12105_16988
Repisalud
author
Fernández-Fernández, Cristina
author
Callado, Luis F
author
Girón, Rocío
author
Sánchez, Eva
author
Erdozain, Amaia M
author
López-Moreno, José Antonio
author
Morales, Paula
author
Rodríguez de Fonseca, Fernando
author
Fernández-Ruiz, Javier
author
Goya, Pilar
author
Meana, J Javier
author
Martín, M Isabel
author
Jagerovic, Nadine
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.
2024-01-15T18:17:06Z
2024-01-15T18:17:06Z
2014-02-20
10.2147/DDDT.S55045
1177-8881
Drug design, development and therapy
http://hdl.handle.net/10668/1607
24591816
http://hdl.handle.net/20.500.12105/17058
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.
eng
Fentanyl
Rimonabant
Cannabinoid
Opioid
Behavioral assays
Autopsia
Cannabinoides
Opioides
moduladores de los receptores de cannabinoides
Encéfalo
Interacciones farmacológicas
Combining rimonabant and fentanyl in a single entity: preparation and pharmacological results.
research article