A microPET comparison of the effects of etifoxine and diazepam on [<sup>11sup>C]flumazenil uptake in rat brains
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- 作者：Caroline Bouillot<sup>asup> ; Fré ; dé ; ric Bonnefoi<sup>asup> ; Franç ; ois Liger<sup>asup> ; Luc Zimmer<sup>asup><sup> ; sup><sup>bsup><sup> ; sup><sup>csup><sup> ; sup><sup>luc.zimmer@univ-lyon1.fr" class="auth_mail" title="E-mail the corresponding authorsup>
- 关键词：Rodent ; Anxiolytic drug ; GABA ; Allosteric site
- 刊名：Neuroscience Letters
- 出版年：2016
- 出版时间：26 January 2016
- 年：2016
- 卷：612
- 期：Complete
- 页码：74-79
- 全文大小：1153 K
文摘
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This study compares [<sup>11sup>C]flumazenil binding to GABA-A receptors in rats after a single injection of etifoxine versus the prototypical benzodiazepine, diazepam, which were both injected at doses reaching pharmacologically active concentrations in the brain.
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A single dose of diazepam produced a significant decrease in the [<sup>11sup>C]flumazenil binding, which can be interpreted as benzodiazepine GABA-A receptor occupancy.
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A single injection of etifoxine increased the [<sup>11sup>C]flumazenil binding, which can be interpreted as an allosteric effect on GABA-A receptors.
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This PET protocol is transferable to human subjects for clinical pharmacology studies.