Estrogen Derivatives for the External Localization of Estrogen-Dependent Malignancy
作者： Richard C. Reba , Haru Kubota , Anneke Mazaitis , Toru Komai , Roger E. Johnsonbaugh
DOI:
关键词: In vivo 、 In vitro 、 Endocrinology 、 Receptor 、 Cytosol 、 Chemistry 、 Estrogen 、 Internal medicine 、 Hexestrol 、 Biochemistry 、 Uterus 、 Hormone receptor
摘要: In an attempt to develop specific diagnostic agents for the detection of hormone-regulated tumors 4 iodinated derivatives estradiol and hexestrol were prepared. Their affinity estrogen-binding protein present in estrogen-response was determined. Structural chemical formulae these compounds are shown. Details technical methods used given. The cytosol rabbit rat uteri used. Competitive-binding experiments sucrose-gradient centrifugation indicated that 1 iodohexestrol binds protein. vitro behavior related vivo distribution. Iodination ortho position A ring interfered with binding Studies immature female rats showed a high uterine uptake at 2 hours. Iodohexestrol also had nonspecific blood cytosol. Thyroxine diminished but prior injection thryoxine increased 2-hour uterus-to-blood ratio from 1.9 10.4. receptor-assay gave good indication distribution receptors.
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