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Synthesis, radiolabeling and in vivo biodistribution of diethylstilbestrol phosphate derivative (DES-P)
Authors:Perihan ünak  F Zümrüt Biber Müftüler  ?i?dem ??hedef  E ?lker Medine  Kübra ?zmen  Turan ünak  Ayfer Yurt Kil?ar  F Gül Gümü?er  Yasemin Parlak  Elvan Say?t Bilgin
Institution:1. Department of Nuclear Applications, Institute of Nuclear Science, Ege University, Bornova, Izmir, Turkey
2. Department of Chemistry, Faculty of Science, Ege University, Bornova, Izmir, Turkey
3. Department of Nuclear Medicine, School of Medicine, Celal Bayar University, Manisa, Turkey
Abstract:Diethylstilbestrol (DES) is a well known, nonsteroidal estrogen with high affinity for the estrogen receptor (ER). Today DES is used to treat breast and prostate cancers. A phosphate derivative of DES Diethylstilbestrol diphosphate (DES-P)] which is specific to tumor cells consisting alkaline phosphatase enzyme was synthesized and labeled with 99mTc using tin chloride as reducing agent. In vivo biological activity of 99mTc labeled diethylstilbestrol phosphate compound (99mTc-DES-P) was examined by biodistribution studies on Wistar Albino rats. Statistical evaluation was performed using SPSS 13 program. The percentage (%) radiolabeling yield of 99mTc-DES-P and quality control studies were done by Thin Layer Radio Chromatography (TLRC). Results showed that, 99mTc-DES-P may be proposed as an imaging agent for ER enriched tumors such as uterus and prostate and their metastases in bones.
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