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首页> 外文期刊>Journal of forensic sciences. >Distribution of venlafaxine, O-desmethylvenlafaxine, and O-desmethylvenlafaxine to venlafaxine ratio in postmortem human brain tissue
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Distribution of venlafaxine, O-desmethylvenlafaxine, and O-desmethylvenlafaxine to venlafaxine ratio in postmortem human brain tissue

机译：文拉法辛，O-去甲基文拉法辛和O-去甲基文拉法辛与文拉法辛比在死后人脑组织中的分布

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摘要

Venlafaxine (VEN) and its metabolite O-desmethylvenlafaxine (ODV) inhibit reuptake of serotonin and norepinephrine. This study examines whether VEN is differentially distributed in postmortem brain and examines relationships between brain and femoral blood concentrations from donors prescribed VEN for treatment of depression. Using high-pressure liquid chromatography-ultraviolet detection, VEN and ODV concentrations were measured in temporal, occipital, and cerebellar cortex of six postmortem brains. The ODV/VEN ratio was calculated as a relative measure of drug metabolism within each region where higher ratios indicated a greater conversion of VEN to ODV. Compared to the other regions examined, the cerebellum showed decreased VEN (p = 0.056), ODV (p = 0.006), and ODV/VEN (p = 0.027) ratios. In parts per million, VEN was higher in temporal and occipital cortex, but not cerebellum, as compared to femoral blood concentration. These observations suggest that VEN and ODV are differentially distributed in the brain, and metabolism of VEN to ODV may vary across brain regions.
机译：文拉法辛（VEN）及其代谢产物O-去甲基文拉法辛（ODV）抑制5-羟色胺和去甲肾上腺素的再摄取。这项研究检查了VEN在死后大脑中是否有差异分布，并检查了处方中指定用于治疗抑郁症的VEN的捐献者的大脑与股骨血药浓度之间的关系。使用高压液相色谱-紫外检测，在六个死后大脑的颞叶，枕叶和小脑皮质中测量VEN和ODV浓度。计算ODV / VEN比率作为每个区域内药物代谢的相对度量，其中较高的比率表明VEN转化为ODV的程度更高。与其他区域相比，小脑的VEN（p = 0.056），ODV（p = 0.006）和ODV / VEN（p = 0.027）比率降低。与股骨血药浓度相比，VEN在颞叶和枕叶皮质中更高，但在小脑中不高。这些观察结果表明VEN和ODV在大脑中的分布不同，并且VEN到ODV的代谢可能在整个大脑区域有所不同。

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