Pastakia B, Lieberman L M, Gatley S J, Young D, Petering D H, Minkel D
J Nucl Med. 1980 Jan;21(1):67-70.
The antitumor activity of, 3-ethoxy-2-oxobutyraldehyde bis (thiosemicarbazone) (KTS), is related to the presence of copper(II) ion. We have studied the tissue distribution of Cu-64-labeled KTS in rats and mice carrying transplanted tumors to evaluate whether the uptake of the radioactivity in the tumor is adequate to warrant further investigation of the tracer as a tumor-seeking agent in patients. Four groups of three of four animals each were studied: (a) mice with fibrosarcoma; (b) mice with mammary adenocarcinoma; (c) rats with fibrosarcoma; and (d) rats with squamous cell carcinoma of the lung. The animals were killed at intervals of 0.25, 1, 4, 24, and 48 hr after i.v. injection of 1.6 X 10(-3) M Cu.KTS containing 3 to 18 muCi Cu-64. Blood, tumor, and six to ten additional tissues were counted for radioactivity. The mouse fibrosarcoma concentrated Cu-64, reaching 15% of the administered dose/g at 48 hr after injection. This suggests that for tumor scanning, the 61.7-hr Cu-67 might be more suitable as a label for KTS than the 12.7-hr Cu-64.
3-乙氧基-2-氧代丁醛双（硫代半卡巴腙）（KTS）的抗肿瘤活性与铜（II）离子的存在有关。我们研究了携带移植瘤的大鼠和小鼠体内铜-64标记的KTS的组织分布，以评估肿瘤中放射性的摄取是否足以保证进一步研究该示踪剂作为患者肿瘤寻踪剂的可能性。研究了四组，每组三只或四只动物：（a）患有纤维肉瘤的小鼠；（b）患有乳腺腺癌的小鼠；（c）患有纤维肉瘤的大鼠；（d）患有肺鳞状细胞癌的大鼠。在静脉注射含3至18微居里铜-64的1.6×10⁻³M铜-KTS后，分别在0.25、1、4、24和48小时的时间间隔处死动物。对血液、肿瘤以及另外六至十个组织进行放射性计数。小鼠纤维肉瘤聚集了铜-64，在注射后48小时达到给药剂量的15%/克。这表明，对于肿瘤扫描，61.7小时的铜-67可能比12.7小时的铜-64更适合作为KTS的标记物。
