新型螯合剂H-73-10的碳-l4和氚标记合成法
LABELLING OF NEW CHALATING AGENT(H-73-10) WITH TRITIUM AND CARBON-14
-
摘要: 新型螯合剂H-73-10是用于促排放射性核素:钚,钍和铀等的,其效果显著优于二十余年居于首位的 Ca-DTPA。通过鼠,狗和猴的急性、亚急性毒性实验,其毒性不高于Ca-DTPA。为了研究此新药在动物体内的药代动力学,进行了碳-14和氚的标记。碳-14的标记方法,采用甲醛-~(14)C与四乙烯五胺和1,2-二羟基苯-3.5-二磺酸钠在冰乙酸溶液中反应。合成~(14)C-H-73-10的比活性为1.02μCi/mg,放化收率为43%。氚标记方法,采用放电曝射法进行不定位标记,比活性55μCi/mg;利用放电曝射法氚标记1,2-二羟基苯-3,5-二磺酸钠,再与四乙烯五胺和甲醛反应。合成定位标记的~3H-H-73-10,比活性为 9.8μCi/mg,放化收率为50%。Abstract: A new chalating agent is used to accelerate excretion of radioactive nucleiPu, Th and U from animal body. The effect of the new medicine is better thanCa-DTPA. Results of acute and subacute toxicity tests on mice, dog and monkey,and a series of pharmaceutical tests showed that the toxicity of the new medicineis not larger than Ca-DTPA. The new chelating agent labelled by ~3H and ~(14)C isused for the study on the absorption, distribution, metabolism and excretion ofmice. ~(14)C-H-73-10(n) is composed of ~(14)C-formal tetraethylene pentamine and1,2-dihydroxybenzene-3, 5-disulphonic acid salt. Specific activity of the productis 1.02μCi/mg. Its radiochemical yield is over 4.3%. ~3H-H-73-10(n) is composedof ~3H-1,2-dihydroxybenzene-3, 5-disulphonic acid salt, tetraethylene pentamineand formal. Its specific activity is 9.8 μCi/mg and radiochemical yield over50%. ~3H-H-73-10(G) is prepared by electric-discharge method with a specificactivity of 55 μCi/mg.