Title |
Combining rimonabant and fentanyl in a single entity: preparation and pharmacological results
|
---|---|
Published in |
Drug Design, Development and Therapy, February 2014
|
DOI | 10.2147/dddt.s55045 |
Pubmed ID | |
Authors |
Cristina Fernández-Fernández, Luis F Callado, Rocío Girón, Eva Sánchez, Amaia M Erdozain, José Antonio López-Moreno, Paula Morales, Fernando Rodríguez de Fonseca, Javier Fernández-Ruiz, Pilar Goya, J Javier Meana, M Isabel Martín, Nadine Jagerovic |
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. |
X Demographics
Geographical breakdown
Country | Count | As % |
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Spain | 1 | 100% |
Demographic breakdown
Type | Count | As % |
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Members of the public | 1 | 100% |
Mendeley readers
Geographical breakdown
Country | Count | As % |
---|---|---|
United States | 2 | 4% |
Unknown | 46 | 96% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Ph. D. Student | 11 | 23% |
Researcher | 9 | 19% |
Student > Bachelor | 5 | 10% |
Other | 4 | 8% |
Professor | 2 | 4% |
Other | 10 | 21% |
Unknown | 7 | 15% |
Readers by discipline | Count | As % |
---|---|---|
Chemistry | 9 | 19% |
Agricultural and Biological Sciences | 6 | 13% |
Pharmacology, Toxicology and Pharmaceutical Science | 5 | 10% |
Medicine and Dentistry | 4 | 8% |
Biochemistry, Genetics and Molecular Biology | 3 | 6% |
Other | 9 | 19% |
Unknown | 12 | 25% |