Desombre E R, Pribish J, Hughes A
Ben May Institute, University of Chicago, IL 60637, USA.
Nucl Med Biol. 1995 Jul;22(5):679-87. doi: 10.1016/0969-8051(95)00002-f.
The uptake, retention and tissue to blood ratios of two non-steroidal, 125I-labeled iodoestrogens, an iodotrihydroxyphenylethylene, 2-iodo-1,2-bis(4-hydroxyphenyl)-2-(3-hydroxyphenyl)ethylene and an iododihydroxyphenylethylene, 2-iodo-1,1-bis(4-hydroxyphenyl)-2-phenylethylene, were compared after intraperitoneal injection in immature female rats. The iodotrihydroxyphenylethylene showed an unexpectedly prolonged specific retention in estrogen target tissue, lasting up to 72 h. It was rapidly cleared from blood and non-target tissues so that uterus or ovary to blood ratios of greater than 100 were seen at 2 and 3 days. This iodotrihydroxyphenylethylene may have clinical potential for estrogen receptor-containing cancers.
在未成熟雌性大鼠腹腔注射两种非甾体类、125I标记的碘雌激素（一种碘代三羟基苯乙烯，2-碘-1,2-双(4-羟基苯基)-2-(3-羟基苯基)乙烯和一种碘代二羟基苯乙烯，2-碘-1,1-双(4-羟基苯基)-2-苯乙烯）后，比较了它们的摄取、滞留以及组织与血液的比率。碘代三羟基苯乙烯在雌激素靶组织中显示出意外延长的特异性滞留，持续长达72小时。它从血液和非靶组织中迅速清除，因此在第2天和第3天观察到子宫或卵巢与血液的比率大于100。这种碘代三羟基苯乙烯可能对含雌激素受体的癌症具有临床潜力。
