Zonisamide的放射标记用于诊断。

IF 1.5 4区 医学 Q3 PHARMACOLOGY & PHARMACY
Emine Dervis, Kadriye Busra Karatay, Kubra Durkan, Ayfer Yurt Kilcar
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引用次数: 0

摘要

目的:癫痫是最古老、最常见的慢性神经系统疾病之一。抗癫痫药物是癫痫治疗的支柱。然而,癫痫发生机制尚未完全阐明。其中一个关键原因是缺乏可靠的生物标志物。神经成像提示了一种非侵入性检查和调查工具,可以检测癫痫发生过程中的关键病理生理变化并监测疾病进展。在目前的研究中,通过促进潜在放射性示踪剂的开发,检测了唑尼酰胺(ZNS)(第二代AED)与锝-99m(99mTc)的放射性标记潜力,以对致痫过程进行神经成像。方法:用99mTc标记ZNS,用薄层液相色谱和高效液相色谱法测定其放射化学产率。通过SHSY5Y人神经母细胞瘤细胞对[999mTc]Tc-ZNS的时间依赖性摄取来测定[999mTc]Tc-ZNS在体外的行为。结果:根据放射色谱研究结果,99mTc]Tc-ZNS的放射化学产率为98.03±1.24%(n=6)。在人神经母细胞瘤SH-SY5Y细胞系上,99mTc]Tc-ZNS在120分钟和240分钟时的摄取值分别是对照组的5.38和6.18倍。结论:本研究表明,目前放射性标记的抗癫痫药物在神经过程成像中具有诊断潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Radiolabeling of Zonisamide for a Diagnostic Perspective.

Objective: 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-99m (99mTc) is examined to neuroimage the epileptogenic processes by contributing to the development of potential radiotracers.

Methods: ZNS was labeled with 99mTc and the radiochemical yield of [99mTc]Tc-ZNS was determined with TLRC (Thin Layer Liquid Radio Chromatography and HPLRC (High Performance Liquid Radio Chromatography) radiochromatographic methods. In vitro behavior of [99mTc]Tc-ZNS was determined with time-dependent uptake of [99mTc]Tc-ZNS on the SHSY5Y human neuroblastoma cells.

Results: The radiochemical yield of [99mTc]Tc-ZNS was determined as 98.03 ± 1.24% (n = 6) according to radiochromatographic studies results. [99mTc]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.

Conclusion: This study showed that the current radiolabeled antiepileptic drug has a diagnostic potential to be used in imaging neurological processes.

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来源期刊
Current radiopharmaceuticals
Current radiopharmaceuticals PHARMACOLOGY & PHARMACY-
CiteScore
3.20
自引率
4.30%
发文量
43
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