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Radiolabeling of lacosamide using highly purified rhenium-188 as a prospective brain theranostic agent

Nuclear Science and Techniques 2020年第10期31卷 105-114页

作者： H.A.El-Sabagh M.I.Aydia A.M.Amin K.M.El-Azony Labeled Compound Department Radioisotopes Production DivisionHot Laboratory CenterAtomic Energy AuthorityP.O.Box 13759 CairoEgypt Radioactive Isotopes and generators Department Radioisotopes Production DivisionHot Laboratory CenterAtomic Energy AuthorityP.O.Box 13759 CairoEgypt

Rhenium-188 is prospectively effective for both diagnosis and radiotherapy as it appropriately emits gamma rays and beta ***(LCM)is a newly approved antiepileptic medication for focal drug-resistant ***-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 *** of 188re-LCM in normal Swiss albino mice was investigated to determine its utility as a potential brain therapy *** 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 *** 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 *** analysis showed that 188re-LCM was primarily localized in the brain(5.1%)with a long residence time(240 min).

关键词： Lacosamide 188re 188w/188re generator Radiolabeling

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