KIH-802，一种2-硝基咪唑的乙酰氧肟酸衍生物，作为一种新型强效低氧细胞放射增敏剂：放射增敏活性、急性毒性及药代动力学
KIH-802, an acetohydroxamic acid derivative of 2-nitroimidazole, as a new potent hypoxic cell radiosensitizer: radiosensitizing activity, acute toxicity, and pharmacokinetics.
作者信息
Sasai K, Shibamoto Y, Takahashi M, Zhou L, Hori H, Nagasawa H, Shibata T, Inayama S, Abe M
机构信息
Department of Radiology, Faculty of Medicine, Kyoto University, Japan.
出版信息
Cancer Chemother Pharmacol. 1990;26(2):112-6. doi: 10.1007/BF02897255.
The radiosensitizing activity, acute toxicity, and pharmacokinetics of a new hypoxic cell radiosensitizer, potassium 2-nitroimidazole-1-acetohydroxamate (KIH-802), were compared with those of misonidazole (MISO) and etanidazole (SR-2508). The radiosensitizing activity of KIH-802 was slightly higher than that of MISO and SR-2508 in vitro and was similar to or slightly higher than that of MISO or SR-2508 in vivo. The acute toxicity of KIH-802 was slightly higher than that of MISO. The concentrations of KIH-802 in the brains and peripheral nerves of mice were as low as those of SR-2508 and lower than those of MISO.
将新型低氧细胞放射增敏剂2-硝基咪唑-1-乙酰氧肟酸钾（KIH-802）的放射增敏活性、急性毒性和药代动力学与甲硝唑（MISO）和依他硝唑（SR-2508）进行了比较。KIH-802的放射增敏活性在体外略高于MISO和SR-2508，在体内与MISO或SR-2508相似或略高。KIH-802的急性毒性略高于MISO。KIH-802在小鼠脑和外周神经中的浓度与SR-2508一样低，且低于MISO。
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