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• W2108573057 abstract "Background: Two 99m Tc-DTPA attached estrone derivatives were synthesized and their radiopharmaceutical potential was determined using female albino Wistar rats. Materials and Methods: Two novel radiolabeled estrone derivatives, 99m Tc-2,2',2'',2'''-(2,2'-(2-(3-methoxy-13-methyl-17- oxo-7,8,9,11,12, 13,14,15,16,17-d ecahydro-6H- cyclopenta(a)phenanthren-2-ylamino)-2-oxoethylazanediyl) bis(ethane-2,1-diyl))bis(azanetriyl) tetraacetic acid ( 99m Tc-2- DTPA-3-methoxy estrone) and 99m Tc-2,2',2'',2'''-(2,2'-(2-(3- methoxy-13-methyl-17-oxo-7,8,9,11,12,13,14,15,16,17-decahydro- 6H-cyclopenta(a)phenanthren-4-ylamino)-2-oxoethylazanediyl) bis(ethane-2,1-diyl))bis(azanetriyl)tetraacetic acid ( 99m Tc-4- DTPA-3-methoxy estrone) were synthesized starting from estrone (3-hydroxy-13-methyl-7,8, 9,11,12,13,15,16-octahydro-6H-cyclo- penta(a)phenanthren-17(14H)-one) and DTPA anhydride (2-(bis(2-(2,6-dioxomorpholino)ethyl)amino)acetic acid) as potential estrogen receptor imaging agents. The products were crystallized in ethyl alcohol (95%), purified by high performance liquid chromatography (HPLC) and characterized by nuclear magnetic resonance (NMR) and infrared spectroscopy (IR). The effect of the radiolabeled compounds on the biological behaviour of the molecules was evaluated through biodistribution studies in female albino Wistar rats. The rats were sacrificed at various time intervals, their organs were removed, and the activities of organs were counted using a gamma counter equipped with a Cd(Te) solid state detector. Results and Conclusion: Organ uptake was calculated as activity/gram tissue and time versus activity curves were generated. The tissue distribution studies exhibited a receptor-mediated uptake in the target organs of the rats for each compound. Both 99m Tc-2-DTPA-3-methoxy estrone and 99m Tc- 4-DTPA-3-methoxy estrone were stable in vitro and were mainly excreted through the hepatobiliary pathway. The biological data showed that the 99m Tc-2-DTPA-3-methoxy estrone had higher uptake in the target tissues than the 99m Tc-4-DTPA-3-methoxy estrone. The favourable in vitro/in vivo stability and biodistribution profiles suggest that these radioligands are good candidates for further exploration of their potential clinical applications. Estrogen compounds are important tools in medicine, especially for estrogen receptor (ER) positive breast and uterine carcinomas and with respect to the preparation of radiopharmaceutics for imaging and treatment (1-6, 7). The determination of estrogen receptor status in human tumors has been shown to improve the selection of patients who may benefit from hormonal therapy and to predict" @default.
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• W2108573057 date "2008-01-01" @default.
• W2108573057 modified "2023-10-17" @default.
• W2108573057 title "Synthesis and Biodistribution Studies of Two Novel Radiolabeled Estrone Derivatives" @default.
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