2014 Feb 20;8:263-77. doi: 10.2147/DDDT.S55045. eCollection 2014.
Combining rimonabant and fentanyl in a single entity: preparation and pharmacological results.
Fernández-Fernández C1, Callado LF2, Girón R3, Sánchez E3, Erdozain AM2, López-Moreno JA4, Morales P1, Rodríguez de Fonseca F5,Fernández-Ruiz J6, Goya P1, Meana JJ2, Martín MI3, Jagerovic N1.
Abstract
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.
KEYWORDS:
behavioral assays, cannabinoid, fentanyl, opioid, rimonabant
- PMID:
- 24591816
- [PubMed – in process]
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