[一种2-硝基咪唑异羟肟酸酯（KIN-804）对小鼠肿瘤的放射增敏作用]

[Radiosensitizing effect of a 2-nitroimidazole hydroxamate (KIN-804) to murine tumors].

作者信息

Tada T, Nakajima T, Onoyama Y, Nagasawa H, Hori H, Inayama S

机构信息

Department of Radiology, Osaka City University Medical School.

出版信息

Nihon Igaku Hoshasen Gakkai Zasshi. 1992 May 25;52(5):688-90.

PMID:1508643

Abstract

We studied the toxicity, pharmacokinesis and radiosensitizing effect of a newly developed 2-nitroimidazole-1-methylacetohydroxamate (KIN-804) in C3H/He mice bearing SCC-VII tumor. They were compared with misonidazole. LD50/7 of KIN-804 and misonidazole were 3200 and 2000 mg/kg. The concentration of KIN-804 in the brain and sciatic nerve was at a very low level and its clearance from the sciatic nerve was rapid. Enhancement ratios calculated using the growth delay method were 1.50 for KIN-804 and 1.36 for misonidazole respectively when they were administered by intraperitoneal injection with a dose of 100 mg/kg. KIN-804 was considered to be a promising radiosensitizer because it obtained less toxicity and a higher radiosensitizing activity than misonidazole.

摘要

我们研究了一种新开发的2-硝基咪唑-1-甲基乙酰氧肟酸酯（KIN-804）对携带SCC-VII肿瘤的C3H/He小鼠的毒性、药代动力学和放射增敏作用。将它们与米索硝唑进行比较。KIN-804和米索硝唑的LD50/7分别为3200和2000 mg/kg。KIN-804在脑和坐骨神经中的浓度非常低，且其从坐骨神经中的清除速度很快。当以100 mg/kg的剂量腹腔注射时，使用生长延迟法计算的增强率KIN-804为1.50，米索硝唑为1.36。KIN-804被认为是一种有前景的放射增敏剂，因为它比米索硝唑毒性更小且放射增敏活性更高。