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多巴胺D2激动剂的非无水性,最基本的合成[18F]MCL-52424
James A H Inkster1,2, Anna W Sromek2,3, Vamsidhar Akurathi1,2
1Division of Nuclear Medicine and Molecular Imaging, Boston Children's Hospital, 300 Longwood Ave., Boston, MA 02115, USA.
Chemistry (Basel, Switzerland)
|October 13, 2023
概括
为PET标记物[18F]MCL-524开发了一种新的合成方法. 这种"无水,最低限度基本"的方法简化了这个过程,可能有助于精神分裂症的研究.
科学领域:
- 放射化学 放射化学是指辐射化学.
- 神经科学是一个神经科学.
- 药理学 药理学是指药理学的学科.
背景情况:
- 在高亲和状态 (D2high) 中的多巴胺D2受体与精神分裂症有关.
- 定子发射断层扫描 (PET) 追踪器[18F]MCL-524针对的是D2高受体.
- 以前的[18F]MCL-524的合成很难复制,缺乏细节.
研究的目的:
- 开发一种可复制和详细的PET追踪器[18F]MCL-524的合成.
- 为了利用一本小说.
- 非无水的,最低限度的基本的.
- (NAMB) 方法用于改进合成.
- 促进研究D2高受体在神经系统疾病中的作用.
主要方法:
- 开发了一种NAMB方法,用于使用甲基酸的[18F]化物化.
- 直接与化前体与化物反应,而无需进行亚热热的干燥.
- 采用三甲酸 (三甲酸) (三甲酸) (三甲酸) (三甲酸) (三甲酸) (三甲酸) (三甲酸) (三甲酸) (三甲酸) (三甲酸) (三甲酸) (三甲酸) (三甲酸) (三甲酸) (三甲酸) (三甲酸) (三甲酸) (三甲酸) (三甲酸) (三甲酸) (三甲酸)),以有效地降低甲基醇的保护作用.
主要成果:
- 通过NAMB方法获得了[18F]MCL-524,其放射性化学产量为5-9% (腐蚀校正).
- 易斯酸降低保护简化了通过HPLC去除副产品,消除了SPE.
- 合成证实可以在多次运行中重现 (n=3).
结论:
- 开发的NAMB方法为[18F]MCL-524提供了改进的,高效的合成.
- 这种方法简化了放射性追踪器的生产和净化.
- NAMB方法可能适用于合成其他标记为18F的放射性追踪剂.
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