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Radiolabeling of lacosamide using highly purified rhenium-188 as a prospective brain theranostic agent 被引量:1
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作者 H.A.El-Sabagh m.i.aydia +1 位作者 A.M.Amin K.M.El-Azony 《Nuclear Science and Techniques》 SCIE CAS CSCD 2020年第10期105-114,共10页
Rhenium-188 is prospectively effective for both diagnosis and radiotherapy as it appropriately emits gamma rays and beta particles.Lacosamide(LCM)is a newly approved antiepileptic medication for focal drug-resistant e... Rhenium-188 is prospectively effective for both diagnosis and radiotherapy as it appropriately emits gamma rays and beta particles.Lacosamide(LCM)is a newly approved antiepileptic medication for focal drug-resistant epilepsy.Rhenium-188 was separated with high elution yield and high purity using the new 188W/188Re generator based on the ZrSiW gel matrix.188Re-LCM was prepared with high radiochemical yield and high purity.Biodistribution of 188Re-LCM in normal Swiss albino mice was investigated to determine its utility as a potential brain therapy agent.The 188W/188Re generator was used to obtain 188Re based on the ZrSi188W gel matrix,and the chemical,radiochemical,and radionuclidic purity of the obtained 188Re was determined using inductively coupled plasma optical emission spectrometry(ICP-AES),a paper chromatography technique,and high-purity germanium(HPGe)detection,respectively,to assess its validity for LCM labeling.Various factors,such as the pH,reaction time,and LCM quantity,were therefore studied in order to improve the yield and purity of 188Re-LCM,as determined by various chromatographic techniques such as electrophoresis,thin layer chromatography(TLC),and highpressure liquid chromatography(HPLC).188Re was obtained with a high elution yield(75±3%)and a low 188W breakthrough(0.001±0.0001%).The maximum radiochemical yield of 188Re-LCM(87.5±1.8%)was obtained using 50 ll LCM(4 mM),250 ll stannous chloride(4.4 mM)at pH 4,100 ll 188Re(37 MBq),within 30 min,at room temperature(25±3C),as determined by TLC,electrophoresis,and HPLC techniques.Biodistribution analysis showed that 188Re-LCM was primarily localized in the brain(5.1%)with a long residence time(240 min). 展开更多
关键词 LACOSAMIDE 188Re 188W/188Re generator RADIOLABELING
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