Japanese
Title99mTc標識多価, 蛋白分解酵素阻害剤, トラジロールのエールリッヒ担癌マウスにおける体内分布についての研究
Subtitle原著
Authors伊藤和夫*, 小林真*, 安東醇**, 利波紀久*, 久田欣一*
Authors(kana)
Organization*金沢大学医学部核医学講座, **金沢大学医療技術短期大学
Journal核医学
Volume13
Number4
Page459-467
Year/Month1976/8
Article原著
Publisher日本核医学会
Abstract「I. 緒言」これまで様々な腫瘍親和性放射性医薬品の開発と研究が報告されて来たが, いまだその集積機序に関しては不明な点も多く, また特異性に欠ける場合のある事が指摘されている. かつて, 悪性腫瘍へfibrinogenが沈着する事を利用して, γ線放射ラジオアイソトープ(RI)にて標識した131I-fibrinogen及び131I-fibrinogen antibodyが悪性腫瘍陽性描画のRI医薬品として報告された. これについては, 安東及び久田等が, すでに報告している. 悪性腫瘍組織の有する凝固能及び組織線維素溶解(以下組織線溶と略す)活性に関しては, 悪性腫瘍の発育と転移機序の解明から興味がもたれ, 田中等が詳細は研究を報告している. 今回, 我々が標識に用いたトラジロールは, その薬理作用の一つとして直接的な組織プラスミン及びアクチベーター阻害作用を有し, 線溶現象の抑制剤として作用する事が知られている. 従って, トラジロールは組織線溶活性が異常な値を示すある種の悪性腫瘍及び血栓形成部位へ集積する可能性が推定され標識化によって, 新しい腫瘍親和性医薬品として使用出来る可能性が予想される.
Practice臨床医学：一般
Keywords
English
TitleBiologic Distribution of 99mTC-Labelled Trasylol in Tumor-Bearing Mice.
SubtitleOriginal Articles
AuthorsKazuo ITOH, Shin KOBAYASHI, Norihisa TONAMI, Kinichi HISADA*,***, Atsushi ANDO**
Authors(kana)
Organization
JournalThe Japanese Journal of nuclear medicine
Volume13
Number4
Page459-467
Year/Month1976/8
ArticleOriginal article
PublisherTHE JAPANESE SOCIETY OF NUCLEAR MEDICINE
Abstract[Summary] The authors have labelled the proteinase inhibitor, Trasylol, with 99mTc-technetium as a new radiopharmaceutical for the detection of malignant neoplasms. Trasylol is a drug used at present in acute pancreatitis and secondary fibrinolysis, which has the direct inhibition effect of the tissue plasminogen activity as one of it's own pharmacological properties. Therefore, it is assumed that 99mTc- labelled Trasylol may accumulate into the abnormal tissues with the high tissue plasminogen activity, e.g., some sorts of the malignant neoplasmas and venous thrombosis. This paper describes the labelling method, the separation, the labelling yield and the chemical stability of labelled compound and the biologic distribution of 99mTc-labelled Trasylol in verious tissue of Ehrlich solid tumor-bearing mice following the intravenous injection. 99mTC-Trasylol was prepared by reducing 99mTc-pertechnetate with Trasylol in HCI solution resolving stannous chloride. The ratio of weight of Trasylol to stannous chloride was 1000:1. The labelling yield of this labelled compound was approximately 75% by Sephadex G-25M (0.9×30 cm column) in 0.9 W/V% NaCl eluent. The chemical stability of labelled compound eluted within void volume was not changed until four hours. The biologic distribution in tumor-bearing male mice was determined at 1 huor, 3 hours, 6 hours and 24 hours following the intravenous injection into the tail vein. The radioactive concentration of 99mTC-Trasylol in various tissues was described as percentage dose per gm. of fresh tissue dirived from five or six mice at each point. Tumor concentration was 1.9715+-0.3277 (mean value +- s.e.m.) at 1 hour and did not change to be constant until 24 hours. Total accumulation of 99mTc- Trasylol to both of the liver and kidney until 1 hour was calculated about 42.8%-33.3% per the administration. Tumor to blood concentration ratio was increased continuously in course of time and became more than 1.0 at 6 hours. 99mTc- Trasylol clearly showed the affinity to the Ehrlich solid tumor but was poorer than the affinity of 99mTc-albumin to the same tumor at 1 hour and 3 hours which we studied as to standard tumorseaking agent. Blood clearance of 99mTc-trasylol, however, was more prompt than that of 99mTc-albumin. Therefore, if it is assumed reasonable that the affinity of 99mTc-Trasylol to tumor tissue is due to the abnormally increased tissue plasmin activity and/or tissue activator activity, it is proposed that 99mTC-trasylol Concentrates the lesion with the active fibrinolysis, some sorts of malignant neoplasms and venous thrombosis, so that we may use it as a new radiopharmaceutical for the diagnosis of such lesions.
PracticeClinical medicine
Keywords

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