Synthesis of 131I labeled estrone derivatives and biodistribution studies on rats

被引：13

作者：

Enginar, H ^{[1
]}

Unak, P

Lambrecht, FY

Biber, FZ

Medine, EI

Cetinkaya, B

机构：

[1] Afyon Kocatepe Univ, Dept Chem, Afyon, Turkey

[2] Ege Univ, Inst Nucl Sci, Dept Nucl Applicat, TR-35100 Izmir, Turkey

来源：

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY | 2005年 / 264卷 / 03期

关键词：

D O I：

10.1007/s10967-005-0749-y

中图分类号：

O65 [分析化学];

学科分类号：

070302 ; 081704 ;

摘要：

The aim of this study is to synthesize novel I-131 labeled estrone derivatives that may have therapeutical potentials on Estrogen Receptor rich tumors. Two radiolabeled estrone derivatives, [I-131]2-iodo-3-methoxy-estra-1,3,5-trien-17-one and [I-131]4-iodo-3-methoxy-estra-1,3,5-trien-17-one were synthesized. Ether amino estrone derivatives were obtained from estrone in three steps by means of diazonium compounds. Tissue distribution studies exhibited receptor-mediated uptake in target organs in female Albino Wistar rats. Maximum uptakes for 2-iodo[I-131]-3-methoxy-estrone are in stomach, pancreas, intestines and uterus. A similar biodistribution profile was obtained for 4-iodo[I-131]-3-methoxy-estrone. However 2-iodo-3-methoxy-estra-1,3,5-trien-17-one has higher uptake in stomach, kidneys, pancreas, and intestines than 4-iodo-derivative.

引用

页码：535 / 539

页数：5

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