Publication: The clobazam metabolite N-desmethyl clobazam is an α2 preferring benzodiazepine with an improved therapeutic window for antihyperalgesia
The clobazam metabolite N-desmethyl clobazam is an α2 preferring benzodiazepine with an improved therapeutic window for antihyperalgesia
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Ralvenius, W. T., Acuña, M. A., Benke, D., Matthey, A., Daali, Y., Rudolph, U., Desmeules, J., Zeilhofer, H. U., & Besson, M. (2016). The clobazam metabolite N-desmethyl clobazam is an α2 preferring benzodiazepine with an improved therapeutic window for antihyperalgesia. Neuropharmacology, 109, 366–375. https://doi.org/10.1016/j.neuropharm.2016.07.004
Abstract
Abstract
Abstract
Data from genetically modified mice suggest that benzodiazepine (BDZ)-site agonists with improved selectivity for α2-subtype GABAA receptors (α2GABAAR) are potentially useful for the treatment of neuropathic pain. Subtype-selective compounds available for preclinical tests in rodents support this concept but have not been approved for human use, hindering proof-of-concept studies in patients. We recently proposed that N-desmethyl clobazam (NDMC), the main metabolite of the licensed BDZ clobazam (CBZ), is responsible for most of the an
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Creators (Authors)
- Ralvenius, William T
- Acuña, Mario A
- Benke, Dietmar
- Matthey, Alain
- Daali, Youssef
- Rudolph, Uwe
- Desmeules, Jules
- Besson, Marie
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Citations
Ralvenius, W. T., Acuña, M. A., Benke, D., Matthey, A., Daali, Y., Rudolph, U., Desmeules, J., Zeilhofer, H. U., & Besson, M. (2016). The clobazam metabolite N-desmethyl clobazam is an α2 preferring benzodiazepine with an improved therapeutic window for antihyperalgesia. Neuropharmacology, 109, 366–375. https://doi.org/10.1016/j.neuropharm.2016.07.004
