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TA—101是一种亲水性三氮唑酰胺的衍生物.采用中国仓鼠V_(79)细胞,通过方便的形成克隆的方法评价了它的增敏活性,而且和Adams教授所赠送的MISO进行了比较.用~(60)CO7射线源照射,剂量率为0.936GY/min.增敏比(OER)由用药则无药时的存活曲线的D_(37)剂量计算.该实验的氧增比(OER)为2 5.接种效率为80±5%.TA—101的浓度为O.2,1.0和2.0mM时其 ERS,分别为1.49,2.05和2.3.实验结果表明0. 2mM TA—101无细胞毒性.TA—101的同类物即使使用5mM也未必察到明显毒性,因此TA—101.是一种有潜力的乏氧细胞辐射敏化剂.
TA-101 is a hydrophilic derivative of trizolamide, and its sensitizing activity was assessed by convenient formation of clones using Chinese hamster V79 cells, and was performed with MISO donated by Professor Adams (OER) was calculated from the dose of D_ (37) of the survival curve without drug.Intra oxygen increased ratio (OER) was 2 5. The inoculation efficiency was 80 ± 5%, and the ERS was 1.49, 2.05 and 2.3 when the concentrations of TA-101 were O.2, 1.0 and 2.0 mM, respectively.Experimental results showed that 0. 2 mM TA-101 No cytotoxicity. TA-101 is a potential hypoxia cell radiosensitizer even though the congener of TA-101 may not be obviously toxic even with 5 mM.