[103Ru]钌茂的氨基酸衍生物的生物化学。与131I马尿酸的比较]
[Biochemistry of amino acid derivatives of [103Ru] ruthenocene. Comparison with 131I hippuran].
作者信息
Wenzel M, Park I H
出版信息
Int J Rad Appl Instrum A. 1986;37(6):491-5. doi: 10.1016/0883-2889(86)90153-x.
The potential radiopharmaceuticals: ruthenocenoyl alanine, ruthenocenoyl methionine, 1'-methyl-ruthenocenoyl glycine and its esters were labelled with 103Ru starting from the analogous ferrocene compounds. In a series of tests in mice and rats these substances were compared with hippuran and ruppuran (= ruthernocenoyl glycine, a ruthenocene-amino acid analogue of hippuran). The organ distribution of these compounds was measured at various times after injection. Kidney concentrations of 1'-methyl-ruthenocenoyl glycine and its esters were found to be extremely high, followed by a rapid excretion. In contrast with these compounds, ruthenocenoyl methionine indicated a significantly greater affinity for liver than for kidney, but not for pancreas. Ruthenocenoyl alanine exhibits a high affinity for tumor cells. The advantages of 97Ru labelled radiopharmaceuticals compared with 99mTc or 123I/131I labelled compounds are discussed.
潜在的放射性药物
钌茂酰丙氨酸、钌茂酰蛋氨酸、1'-甲基钌茂酰甘氨酸及其酯类，是从类似的二茂铁化合物出发，用¹⁰³Ru进行标记的。在对小鼠和大鼠进行的一系列测试中，将这些物质与马尿酸和鲁普尿酸（=钌茂酰甘氨酸，马尿酸的一种钌茂基氨基酸类似物）进行了比较。在注射后的不同时间测量了这些化合物的器官分布。发现1'-甲基钌茂酰甘氨酸及其酯类在肾脏中的浓度极高，随后迅速排泄。与这些化合物不同，钌茂酰蛋氨酸对肝脏的亲和力明显高于对肾脏的亲和力，但对胰腺则不然。钌茂酰丙氨酸对肿瘤细胞表现出高亲和力。讨论了⁹⁷Ru标记的放射性药物与⁹⁹ᵐTc或¹²³I/¹³¹I标记的化合物相比的优势。
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