Complete in vivo reversal of P-glycoprotein pump function in the blood-brain barrier visualized with positron emission tomography
Complete in vivo reversal of P-glycoprotein pump function in the blood-brain barrier visualized with positron emission tomography
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DOI：
10.1038/sj.bjp.0701979
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发表时间：
1998-08-01
影响因子：
7.3
通讯作者：
Franssen, EJF
中科院分区：
文献类型：
--
作者：
Hendrikse, NH;Schinkel, AH;Franssen, EJF
1 使用 mdr1a 基因纯合破坏小鼠（mdr1a(-/-) 小鼠）和野生型小鼠（mdr1a(+/+) 小鼠）开发一种无创 P-糖蛋白（P-gp）功能成像方法，并研究 P-gp 逆转剂对其体内功能的影响。2 给予[C-11]维拉帕米（0.1 mg/kg），观察组织浓度变化通过器官摘除进行离体测定，通过 PET 进行体内测定。为了阻断 P-gp 功能，使用环孢菌素 A。3 生物分布研究显示 9.5 倍（P
1 Homozygously mdr1a gene disrupted mice (mdr1a(-/-) mice) and wild type mice (mdr1a(+/+) mice) were used to develop a method for P-glycoprotein (P-gp) function imaging non-invasively and to study the effect of a P-gp reversal agent on its function in vivo.2 [C-11]verapamil (0.1 mg/kg) was administered and the changes in tissue concentrations were determined ex vivo by organ extirpation and in viva with PET. To block P-gp function, cyclosporin A was administered.3 Biodistribution studies revealed 9.5-fold (P