BMS181321在啮齿动物和人类细胞中的蓄积：P-糖蛋白的作用
BMS181321 accumulation in rodent and human cells: the role of P-glycoprotein.
作者信息
Cowan D S, Melo T, Park L, Ballinger J R, Rauth A M
机构信息
Department of Medical Biophysics, University of Toronto, Canada.
出版信息
Br J Cancer Suppl. 1996 Jul;27:S264-6.
A 2-nitroimidazole with a side chain that contains technetium-99m as a chelate, BMS181321, is undergoing evaluation as an imaging agent for myocardial and cerebral ischaemia, as well as a diagnostic probe for hypoxic cells in solid tumours. Its accumulation in hypoxic and aerobic populations of three lines of Chinese hamster ovary cells of differing P-glycoprotein status, as well as one rat and two human cell lines has been determined. There was selective accumulation of BMS181321 in hypoxic vs aerobic cells. P-glycoprotein level was not a factor in this accumulation and hypoxic human cells accumulated BMS181321 more rapidly than the rodent cells. These results indicate P-glycoprotein levels in tumour cells will not confound the use of BMS181321 as a hypoxic cell marker.
一种带有侧链的2-硝基咪唑，该侧链包含作为螯合物的锝-99m（BMS181321），正在作为心肌和脑缺血的成像剂以及实体瘤中缺氧细胞的诊断探针进行评估。已经测定了它在三种不同P-糖蛋白状态的中国仓鼠卵巢细胞系以及一种大鼠细胞系和两种人类细胞系的缺氧和好氧群体中的积累情况。BMS181321在缺氧细胞与好氧细胞中有选择性积累。P-糖蛋白水平不是这种积累的影响因素，并且缺氧人类细胞比啮齿动物细胞更快地积累BMS181321。这些结果表明肿瘤细胞中的P-糖蛋白水平不会干扰将BMS181321用作缺氧细胞标记物。
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