Dervis Emine, Karatay Kadriye Busra, Durkan Kubra, Kilcar Ayfer Yurt
Department of Nuclear Applications, Institute of Nuclear Sciences, Ege University, Izmir, Turkey.
Curr Radiopharm. 2024;17(1):91-98. doi: 10.2174/0118744710249156231002115024.
Epilepsy is one of the oldest and the most common chronic neurological diseases. Antiepileptic drugs (AEDs) are the backbone of epilepsy treatment. However, epileptogenesis has not been fully elucidated. One of the critical reasons for this is the lack of reliable biomarkers. Neuroimaging suggests a non-invasive examination and investigation tool that can detect critical pathophysiological changes involved in epileptogenesis and monitor disease progression. In the current study, the radiolabeling potential of Zonisamide (ZNS) (the secondgeneration AED) with Technetium- (Tc) is examined to neuroimage the epileptogenic processes by contributing to the development of potential radiotracers.
ZNS was labeled with Tc and the radiochemical yield of [Tc]Tc-ZNS was determined with TLRC (Thin Layer Liquid Radio Chromatography and HPLRC (High Performance Liquid Radio Chromatography) radiochromatographic methods. behavior of [Tc]Tc-ZNS was determined with time-dependent uptake of [Tc]Tc-ZNS on the SHSY5Y human neuroblastoma cells.
The radiochemical yield of [Tc]Tc-ZNS was determined as 98.03 ± 1.24% (n = 6) according to radiochromatographic studies results. [Tc]Tc-ZNS demonstrated 5.38 and 6.18 times higher uptake values than the control group on the human neuroblastoma SH-SY5Y cell line at 120 and 240 minutes, respectively.
This study showed that the current radiolabeled antiepileptic drug has a diagnostic potential to be used in imaging neurological processes.
癫痫是最古老且最常见的慢性神经疾病之一。抗癫痫药物（AEDs）是癫痫治疗的主要手段。然而，癫痫的发病机制尚未完全阐明。其中一个关键原因是缺乏可靠的生物标志物。神经影像学提示了一种非侵入性检查和研究工具，可检测癫痫发病机制中涉及的关键病理生理变化并监测疾病进展。在本研究中，通过助力潜在放射性示踪剂的开发，研究了第二代抗癫痫药物唑尼沙胺（ZNS）与锝（Tc）的放射性标记潜力，以对癫痫发病过程进行神经成像。
用Tc标记ZNS，并采用薄层层析液相放射性色谱法（TLRC）和高效液相放射性色谱法（HPLRC）放射性色谱方法测定[Tc]Tc-ZNS的放射化学产率。通过[Tc]Tc-ZNS在SHSY5Y人神经母细胞瘤细胞上的时间依赖性摄取来确定[Tc]Tc-ZNS的行为。
根据放射性色谱研究结果，[Tc]Tc-ZNS的放射化学产率测定为98.03±1.24%（n = 6）。[Tc]Tc-ZNS在120分钟和240分钟时在人神经母细胞瘤SH-SY5Y细胞系上的摄取值分别比对照组高5.38倍和6.18倍。
本研究表明，当前的放射性标记抗癫痫药物具有用于神经过程成像的诊断潜力。
