Combining rimonabant and fentanyl in a single entity: preparation and pharmacological results
Data(s) |
04/04/2016
04/04/2016
2014
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Resumo |
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 well-known drugs, ie, rimonabant and fentanyl. The new compounds have been tested for their affinity and functionality regarding CB1 and CB2 cannabinoid and mu opioid receptors. In [S-35]-GTP.S (guanosine 5'-O-[gamma-thio] triphosphate) binding assays from the post-mortem human frontal cortex, they proved to be CB1 cannabinoid antagonists and mu opioid antagonists. Interestingly, in vivo, the new compounds exhibited a significant dual antagonist action on the endocannabinoid and opioid systems. |
Identificador |
Drug Design, Development and Therapy 8 2014 : 263-277(2014) // Article ID S55045 1177-8881 http://hdl.handle.net/10810/17779 10.2147/DDDT.S55045 |
Idioma(s) |
eng |
Publicador |
Dove Medical Press |
Relação |
https://www.dovepress.com/combining-rimonabant-and-fentanyl-in-a-single-entity-preparation-and-p-peer-reviewed-article-DDDT# |
Direitos |
© 2014 Fernández-Fernández et al. This work is published by Dove Medical Press Limited, and licensed under Creative Commons Attribution – Non Commercial (unported, v3.0) License. The full terms of the License are available at http://creativecommons.org/licenses/by-nc/3.0/. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. Permissions beyond the scope of the License are administered by Dove Medical Press Limited. Information on how to request permission may be found at: http://www.dovepress.com/permissions.php info:eu-repo/semantics/openAccess |
Palavras-Chave | #fentanyl #rimonabant #cannabinoid #opioid #behavioral assays #postmortem human brain #receptor antagonist SR-141716 #I-2 imidazoline binding-sites #alcohol deprivation #opioid interactions #food-intake #CB1 #rats #ligands #derivatives |
Tipo |
info:eu-repo/semantics/article |