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In silico and in vivo study of radio-iodinated nefiracetam as a radiotracer for brain imaging in mice
Radiochimica Acta ( IF 1.4 ) Pub Date : 2021-07-01 , DOI: 10.1515/ract-2020-0125
M. H. Sanad 1 , A. B. Farag 2 , S. F. A. Rizvi 3
Affiliation  

This study presents development and characterization of a radiotracer, [ 125 I]iodonefiracetam ([ 125 I]iodoNEF). Labeling with high yield and radiochemical purity was achieved through the formation of a [ 125 I]iodoNEF radiotracer after investigating many factors like oxidizing agent content (chloramines-T (Ch-T)), substrate amount (Nefiracetam (NEF)), pH of reaction mixture, reaction time and temperature. Nefiracetam (NEF) is known as nootropic agent, acting as N -methyl- d -aspartic acid receptor ligand (NMDA). The radiolabeled compound was stable, and exhibited the logarithm of the partition coefficient (log p ) value of [ 125 I]iodonefiracetam as 1.85 (lipophilic). Biodistribution studies in normal mice confirmed the suitability of the [ 125 I]iodoNEF radiotracer as a novel tracer for brain imaging. High uptake of 8.61 ± 0.14 percent injected dose/g organ was observed in mice

中文翻译:

放射性碘化奈非西坦作为小鼠脑成像放射性示踪剂的计算机模拟和体内研究

本研究介绍了放射性示踪剂 [ 125 I] 碘非拉西坦 ([ 125 I]iodoNEF) 的开发和表征。在研究了氧化剂含量(氯胺-T(Ch-T))、底物量(奈非西坦(NEF))、pH反应混合物、反应时间和温度。奈非西坦 (NEF) 被称为促智剂,充当 N-甲基-d-天冬氨酸受体配体 (NMDA)。放射性标记的化合物是稳定的,并且表现出[ 125 I]碘非拉西坦的分配系数(log p)值的对数为1.85(亲脂性)。在正常小鼠中的生物分布研究证实了 [ 125 I]iodoNEF 放射性示踪剂作为脑成像的新型示踪剂的适用性。8.61 ± 0 的高吸收率。
更新日期:2021-07-04
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