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关于硝基咪唑类药物亲脂性对体外培养哺乳动物细胞放射增敏作用的快速混合研究。

A rapid-mix study on the effect of lipophilicity of nitroimidazoles on the radiosensitization of mammalian cells in vitro.

作者信息

Watts M E, Hodgkiss R J, Jones N R, Sehmi D S, Woodcock M

出版信息

Int J Radiat Biol Relat Stud Phys Chem Med. 1983 Mar;43(3):329-36. doi: 10.1080/09553008314550371.

DOI:10.1080/09553008314550371
PMID:6601082
Abstract

A liquid flow rapid-mixing apparatus has been used to study the role of lipophilicity (octanol: water partition coefficient, P) in the sensitization of hypoxic V79 cells by nitroimidazoles. Sensitization by seven neutral 2-nitroimidazoles of similar reduction potential but widely differing partition (0.11-77) and one basic 2-nitroimidazole (pKa=8.9; p=8.5 (of free base)) was studied as a function of pre-irradiation contact time ca. 3-40 ms. With increasing P, sensitization occurs at increasingly shorter pre-irradiation contact times. The results suggest that even though factors other than passive diffusion control the sensitization observed with the base Ro 03-8799 it is able to diffuse to the target site faster than midonidazole.

摘要

一种液体流动快速混合装置已被用于研究亲脂性(正辛醇:水分配系数,P)在硝基咪唑对缺氧V79细胞致敏作用中的角色。研究了七种具有相似还原电位但分配系数差异很大(0.11 - 77)的中性2 - 硝基咪唑和一种碱性2 - 硝基咪唑(pKa = 8.9;p = 8.5(游离碱))的致敏作用与预辐照接触时间(约3 - 40毫秒)的关系。随着P的增加,致敏作用在越来越短的预辐照接触时间出现。结果表明,尽管除被动扩散之外的其他因素控制着碱性的Ro 03 - 8799所观察到的致敏作用,但它比米多硝唑能更快地扩散到靶位点。

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A rapid-mix study on the effect of lipophilicity of nitroimidazoles on the radiosensitization of mammalian cells in vitro.关于硝基咪唑类药物亲脂性对体外培养哺乳动物细胞放射增敏作用的快速混合研究。
Int J Radiat Biol Relat Stud Phys Chem Med. 1983 Mar;43(3):329-36. doi: 10.1080/09553008314550371.
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