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氨巯基类辐射防护剂WR-1065(N-2-巯乙基-1,3-二氨基丙烷)是WR-2721的活性部分.实验选用中国仓鼠卵巢AA8(CHOAA8)细胞与37kBq/ml〔~(14)C〕WR-1065共同培养,通过WR-1065生物稳定性的测定及药物与细胞的结合实验,观察了WR-1065是与细胞随机结合的还是特异性的与细胞核及核质体结合.〔~(14)C〕WR-1065掺入细胞的动力学研究表明:药物在最初30分钟内与细胞迅速结合,逐步达到坪值,且坪值段较宽,直至给药后3小时一直缓慢增长,提示药物在细胞内能迅速达到稳定状态;如将
Aminoguanidine-based radioprotectant WR-1065 (N-2-Ethylethyl-1,3-diaminopropane) is the active part of WR-2721. The experiment used Chinese hamster ovary AA8 (CHOAA8) cells and 37kBq/ml [~ (14)C] WR-1065 co-culture, through the determination of WR-1065 biological stability and drug-cell binding experiments, it was observed whether WR-1065 was randomly associated with cells or specific binding to the nucleus and nucleoplasm. A kinetic study of the incorporation of WR-1065 into cells showed that the drug rapidly bound to the cells within the first 30 minutes, gradually reached a plateau, and the plateau was wider until 3 hours after administration. Slow growth, suggesting that the drug can quickly reach a steady state within the cell;