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用于PET成像α-Synuclein的pyridothiophene化合物的开发

Anna Pees¹, Junchao Tong¹, Saritha Birudaraju²

¹Azrieli Centre for Neuro-Radiochemistry, Brain Health Imaging Centre, Campbell Family Mental Health Research Institute, Centre for Addiction and Mental Health (CAMH), Toronto, ON M5T 1R8, Canada.

Chemistry (Weinheim an der Bergstrasse, Germany)

|February 14, 2024

概括

研究人员探索了pyridothiophene化合物作为帕金森病 (PD) 和莱维体痴呆症 (LBD) 的潜在成像剂. 虽然[18F]asyn-44在体外具有前景,但其代谢不稳定,阻碍了进一步的PET成像开发.

科学领域:

神经科学是一个神经科学.
放射化学放射化学是指辐射化学.
药理学药理学是指药理学的学科.

背景情况:

聚合的α-synuclein (α-syn) 是帕金森病 (PD) 和莱维体痴呆症 (LBD) 的关键标志物.
开发用于成像α-syn聚合物的正电子发射断层扫描 (PET) 放射追踪器对于诊断和研究这些神经退行性疾病至关重要.

研究的目的:

评估用于开发新型α-syn PET射线追踪剂的二基基架.
为了合成和表征一种强大的铁二烯化合物,asyn-44的衍生物,以了解它们作为PET成像剂的潜力.

主要方法:

合成了47种pyridothiophene衍生物,并使用 [3H]asyn-44 的竞争性结合试验对它们进行了选.
对于有力的化合物,确定平衡抑制常数 (Ki) 值.
合成了标记为asyn-44 ([18F]asyn-44) 的-18并对老鼠进行了初步的PET成像,包括放射性代谢物分析.

主要成果:

确定了三种具有纳米分子结合亲和度 (Ki值为12-15nM) 的二甲基衍生物.
[3H]asyn-44在PD和多个系统缩捐赠者的脑组织的自身放射学研究中显示出有前途.
[18F]asyn-44在老鼠中表现出良好的初始脑吸收和可接受的生物分布,但观察到显著的放射代谢物形成.

结论:

二甲基基架显示了α-synPET标记物发展的潜力,几个衍生品显示了高亲和力.
[18F]asyn-44在体内PET成像中的实用性受到其代谢不稳定性的限制.
需要进一步优化二衍生物,以实现高亲和度和改善代谢稳定性,以成功对α-syn病理的PET成像.

关键词:

帕金森病是帕金森病的一种.-18 -18 -18 -18 -18 -18 -18 -18 定子发射断层扫描 (PET).α-synuclein 是一种同核蛋白.

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