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Updated: May 2, 2026

Author Spotlight: An Efficient Methodology to Confidently Differentiate and Characterize Fentanyl Analogs
Published on: November 8, 2024
Combining rimonabant and fentanyl in a single entity: preparation and pharmacological results
Cristina Fernández-Fernández1, Luis F Callado2, Rocío Girón3
1Instituto de Química Médica, CSIC, Madrid, Spain.
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.
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