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

Authors Fernández-Fernández C, Callado LF, Girón R, Sánchez E, Erdozain AM, López-Moreno JA, Morales P, Rodríguez de Fonseca F, Fernández-Ruiz J, Goya P, Meana JJ, Martín MI, Jagerovic N

Received 27 September 2013

Accepted for publication 5 November 2013

Published 20 February 2014 Volume 2014:8 Pages 263—277

DOI https://doi.org/10.2147/DDDT.S55045

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 3

Cristina Fernández-Fernández,1 Luis F Callado,2 Rocío Girón,3 Eva Sánchez,3 Amaia M Erdozain,2 José Antonio López-Moreno,4 Paula Morales,1 Fernando Rodríguez de Fonseca,5 Javier Fernández-Ruiz,6 Pilar Goya,1 J Javier Meana,2 M Isabel Martín,3 Nadine Jagerovic1

1Instituto de Química Médica, CSIC, Madrid, 2Departamento de Farmacología, Universidad del Pais Vasco, UPV/EHU, CIBERSAM, Leioa, 3Departamento de Farmacología y Nutrición, Ciencias de la Salud, Universidad Rey Juan Carlos, Alcorcón, 4Departamento de Psicobiologia, Universidad Complutense de Madrid, Madrid, 5Laboratorio de Medicina Regenerativa, Hospital Carlos Haya, Fundación IMABIS, Málaga, 6Departamento de Bioquímica y Biología Molecular, Facultad de Medicina, CIBERNED, IRYCIS, Universidad Complutense de Madrid, 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 [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.


Keywords: fentanyl, rimonabant, cannabinoid, opioid, behavioral assays

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