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Combining rimonabant and fentanyl in a single entity: Preparation and pharmacological results

AuthorsFernández-Fernández, Cristina ; Callado, Luis F.; Girón, Rocío; Sánchez, Eva; Erdozain, Amaia M.; López-Moreno, José Antonio; Morales, Paula ; Rodriguez de Fonseca, Fernando; Fernández-Ruiz, Javier; Goya, Pilar ; Meana, J. Javier; Martín, M. Isabel ; Jagerovic, Nadine
behavioral assays
Issue Date2014
CitationDrug Design, Development and Therapy 8: 263- 277 (2014)
AbstractBased 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 [35S]-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. © 2014 Fernández-Fernández et al.
Identifiersdoi: 10.2147/DDDT.S55045
issn: 1177-8881
Appears in Collections:(IQM) Artículos
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