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[锝-99m标记放射性药物的肿瘤亲和性研究。(2) 99m锝-亚锡二膦酸盐(99m锝-依替膦酸盐)、99m锝-亚锡二巯基丁二酸(99m锝-二巯基丁二酸)和99m锝-亚锡己烯雌酚二磷酸酯(99m锝-己烯雌酚二磷酸酯)]

[Study on tumor affinity of technetium-99m-labeled radiopharmaceuticals. (2) 99mTc-Sn-diphosphonate (99mTc-EHDP), 99mTc-Sn-dimercaptosuccinic acid (99mTc-DMSA), and 99mTc-Sn-diethyl stilbestrol diphosphate (99mTc-DSDP)].

作者信息

Ito K, Kobayashi S, Hisada K, Tonami N, Ando A

出版信息

Radioisotopes. 1976 Oct;25(10):622-9. doi: 10.3769/radioisotopes.25.10_622.

DOI:10.3769/radioisotopes.25.10_622
PMID:1037404
Abstract

The authors have examined the tumor affinity of various 99mTc-labelled radiopharmaceuticals to Ehrlich's tumor for the purpose of delineating positively human malignant neoplasm. This paper includes biologic distributions of 99mTc-Sn-diphosphonate (99mTc-EHDP), 99mTc-Sn-dimercaptosuccinic acid (99mTc-DMSA) and 99mTc-Sn-diethyl stilbestrol diphosphate (99mTc-DSDP, 99mTc-Honvan) as the second report on the tumor affinity to the Ehrlich-bearing mice. (a) Tumor concentration of 99mTc-EHDP was lowest and the positive delineation of implanted tumor with 99mTc-EHDP was poorest in sequential images, though the active accumulation to some soft tissue maglinant neoplasms, the breast cancer and the thyroid cancer, has been reported. (b) Tumor concentration and tumor to blood ratio of 99mTc-DMSA were not so high on the contrary of our expectation that 197Hg-DMSA may show the high tumor concentration and the high tumor to blood ratio like 197Hg chlormerodrin as same renal scanning radiopharmaceuticals. (c) Tumor concentration of 99mTc-DSDP was highest. Tumor to blood concentration ratio, however, was lower than that of the above mentioned radiopharmaceuticals but tumor to liver ratio and/or tumor to lung ratio was over 1.0 at the earlier time. Biologic distribution of 99mTc-DSDP was similar to that of 32P labeled DSDP and then it is presumed that 99mTc is labeled at phosphate ester of DSDP which is dephospholytated immediately by phospholylase in vivo following the intravenous injection. Therefore, it may be assumed that the accumulation mechanism of 99mTc-DSDP to Ehrlich's tumor is related to the phospholylase activity in neoplasms but is not known precisely.

摘要

为了明确诊断人类恶性肿瘤,作者研究了各种99mTc标记的放射性药物对艾氏腹水癌的肿瘤亲和力。本文介绍了99mTc-锡-二膦酸盐(99mTc-EHDP)、99mTc-锡-二巯基丁二酸(99mTc-DMSA)和99mTc-锡-己烯雌酚二磷酸酯(99mTc-DSDP,99mTc-Honvan)的生物学分布,这是关于对荷艾氏腹水癌小鼠肿瘤亲和力的第二篇报告。(a)99mTc-EHDP的肿瘤摄取量最低,在连续图像中用99mTc-EHDP对植入肿瘤的阳性显像最差,尽管已有报道其对某些软组织恶性肿瘤、乳腺癌和甲状腺癌有活性聚集。(b)与我们的预期相反,99mTc-DMSA的肿瘤摄取量和肿瘤与血液的比值并不高,我们原本期望197Hg-DMSA能像用于肾脏扫描的放射性药物197Hg氯汞君一样,显示出高肿瘤摄取量和高肿瘤与血液的比值。(c)99mTc-DSDP的肿瘤摄取量最高。然而,肿瘤与血液浓度的比值低于上述放射性药物,但在早期肿瘤与肝脏的比值和/或肿瘤与肺的比值超过1.0。99mTc-DSDP的生物学分布与32P标记的DSDP相似,因此推测99mTc标记在DSDP的磷酸酯上,静脉注射后在体内被磷酸化酶立即脱磷酸。所以,可以假定99mTc-DSDP在艾氏腹水癌中的聚集机制与肿瘤中的磷酸化酶活性有关,但尚不清楚确切情况。

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