Assessment of regional differences in tariquidar-induced P-glycoprotein modulation at the human blood-brain barrier

Assessment of regional differences in tariquidar-induced P-glycoprotein modulation at the human blood-brain barrier
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DOI:
10.1038/jcbfm.2009.265
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发表时间:
2010-03-01
影响因子:
6.3
通讯作者:
Langer, Oliver
Langer, Oliver
中科院分区:
医学1区
文献类型:
--
作者:
Bauer, Martin;Karch, Rudolf;Langer, Oliver

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` 我们试图通过使用 P-gp 底物 (R)[C-11]维拉帕米对 5 名健康受试者进行静脉注射前后的配对正电子发射断层扫描 (PET) 扫描来评估脑 P-糖蛋白 (P-gp) 功能的区域差异。输注塔利奎达(2 mg/kg)。比较 Tariquidar 引起的 42 个大脑感兴趣区域 (ROI) 中分布体积 (DV) 的变化,未能检测到大脑 ROI 之间的显着差异。参数 DV 图像的统计参数映射分析显示,小脑、海马旁回、嗅回、中颞叶和皮质中出现对称双侧簇,DV 适度升高,这可能反映了 P-gp 功能和表达的适度下降。脑血流与代谢杂志 (2010) 30, 510-515; doi:10.1038/jcbfm.2009.265; 2009 年 12 月 16 日在线发布
` We attempted to assess regional differences in cerebral P-glycoprotein (P-gp) function by performing paired positron emission tomography (PET) scans with the P-gp substrate (R)[C-11]verapamil in five healthy subjects before and after i.v. infusion of tariquidar (2 mg/kg). Comparison of tariquidar-induced changes in distribution volumes (DVs) in 42 brain regions of interest (ROIs) failed to detect significant differences among brain ROIs. Statistical parametric mapping analysis of parametric DV images visualized symmetrical bilateral clusters with moderately higher DV increases in response to tariquidar administration in cerebellum, parahippocampal gyrus, olfactory gyrus, and middle temporal lobe and cortex, which might reflect moderately decreased P-gp function and expression. Journal of Cerebral Blood Flow & Metabolism (2010) 30, 510-515; doi: 10.1038/jcbfm.2009.265; published online 16 December 2009