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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%。
The new chelating agent H-73-10 is used to promote the emission of radionuclides: plutonium, thorium and uranium, the effect is significantly better than Ca-DTPA in more than twenty years. Acute, subacute toxicity studies in rats, dogs and monkeys show no greater toxicity than Ca-DTPA. In order to study the pharmacokinetics of this new drug in animals, carbon-14 and tritium labeling was performed. Carbon-14 labeling method using formaldehyde - ~ (14) C with tetraethylenepentamine and 1,2-dihydroxybenzene-3.5-disulfonate sodium in glacial acetic acid solution. The specific activity of ~ (14) C-H-73-10 was 1.02μCi / mg and the radiochemical yield was 43%. Tritium labeling method, the use of discharge exposure method for the unlocated marker, the specific activity of 55μCi / mg; using discharge exposure tritium labeled 1,2-dihydroxybenzene-3,5-disulfonate sodium, and then tetraethylenepentamine Reacts with formaldehyde. ~ 3H-H-73-10 was synthesized and labeled with a specific activity of 9.8 μCi / mg and the radiochemical yield was 50%.