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新型蒽环类药物ME2303(FAD - 104)的生物学特性

Biological properties of ME2303 (FAD-104), a new anthracycline.

作者信息

Omoto S, Kondo S, Fukatsu S, Takeuchi T, Umezawa K, Tsuchiya T, Umezawa S

机构信息

Meiji Seika Kaisha, Ltd., Tokyo, Japan.

出版信息

Drugs Exp Clin Res. 1988;14(7):435-9.

PMID:3240704
Abstract

ME2303 (FAD-104) is a new anthracycline antibiotic whose structure is characterized by the presence of a 2'-fluoro atom and the lack of a 3'-amino group in the sugar moiety. Its cytocidal activity is superior to or equal to that of adriamycin (ADM). The LD50 value of ME2303 was about 140 mg/kg i.v. in mice and this value was about 7-fold higher than that of ADM. ME2303 was administered intravenously to Golden strain hamsters at doses of 25, 50, 75 and 150 mg/kg and the ECG was examined. From ECG changes, it seems that ME2303 did not show any effect on the heart in acute toxicity. Mutagenicity was recognized as with ADM in the back-mutation test.

摘要

ME2303(FAD - 104)是一种新型蒽环类抗生素,其结构特点是在糖部分存在2'-氟原子且缺少3'-氨基。其杀细胞活性优于或等同于阿霉素(ADM)。ME2303在小鼠体内静脉注射的半数致死量(LD50)约为140mg/kg,该值比阿霉素高约7倍。以25、50、75和150mg/kg的剂量给金黄仓鼠静脉注射ME2303,并检查心电图。从心电图变化来看,ME2303在急性毒性中似乎对心脏没有任何影响。在回复突变试验中,ME2303与阿霉素一样具有致突变性。

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1
Biological properties of ME2303 (FAD-104), a new anthracycline.新型蒽环类药物ME2303(FAD - 104)的生物学特性
Drugs Exp Clin Res. 1988;14(7):435-9.
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Comparison of pharmacokinetics of M1, M2, M3, and M4 after intravenous administration of DA-125 or ME2303 to mice and rats. New adriamycin analogues containing fluorine.给小鼠和大鼠静脉注射DA - 125或ME2303后M1、M2、M3和M4的药代动力学比较。含氟的新型阿霉素类似物。
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Comparison of antitumor activity of new anthracycline analogues, ME2303, KRN8602, and SM5887 using human lung cancer cell lines.使用人肺癌细胞系比较新型蒽环类类似物ME2303、KRN8602和SM5887的抗肿瘤活性
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