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MAO-B 抑制剂并不阻止体内 [F]-AV-1451(flortaucipir)结合。

MAO-B Inhibitors Do Not Block In Vivo Flortaucipir([F]-AV-1451) Binding.

机构信息

Department of Nuclear Medicine and PET-Centre, Institute of Clinical Medicine, Aarhus University, Norrebrogade 44, bld. 10G, DK-8000, Aarhus C, Denmark.

Division of Neuroscience, Department of Medicine, Imperial College London, London, UK.

出版信息

Mol Imaging Biol. 2018 Jun;20(3):356-360. doi: 10.1007/s11307-017-1143-1.

Abstract

PURPOSE

Recent evidence suggests that the tau radiotracer [F]THK-5351 displays high affinity for the monoamine oxidase type B (MAO-B) enzyme. Utilizing another tau-tracer, flortaucipir ([F]AV-1451), we previously reported that non-demented Parkinson's disease patients show off-target binding in subcortical structures, but no appreciable cortical uptake. However, 59 % of these patients were receiving MAO-B inhibitors at the time of their scan. Here, we retrospectively investigated if MAO-B inhibitors in clinical doses affect flortaucipir binding.

PROCEDURES

We compared the standard uptake values of flortaucipir at regional and voxel levels in Parkinson's disease patients who received MAO-B inhibitors with those who did not.

RESULTS

Sixteen of 27 Parkinson's disease patients received MAO-B inhibitors at the time of scan. We found no significant flortaucipir uptake differences between the groups at voxel or regional levels.

CONCLUSION

Use of MAO-B inhibitors at pharmaceutical levels did not significantly affect flortaucipir binding. Thus, MAO-B does not appear to be a significant binding target of flortaucipir.

摘要

目的

最近的证据表明,tau 示踪剂 [F]THK-5351 对单胺氧化酶 B(MAO-B)酶显示出高亲和力。利用另一种 tau 示踪剂,氟托卡比([F]AV-1451),我们之前报道说,非痴呆帕金森病患者在皮质下结构中显示出脱靶结合,但皮质摄取没有明显增加。然而,这些患者中有 59%在扫描时正在服用 MAO-B 抑制剂。在这里,我们回顾性研究了临床剂量的 MAO-B 抑制剂是否会影响氟托卡比的结合。

过程

我们比较了在扫描时接受 MAO-B 抑制剂和未接受 MAO-B 抑制剂的帕金森病患者在区域和体素水平上氟托卡比的标准摄取值。

结果

27 名帕金森病患者中有 16 名在扫描时接受了 MAO-B 抑制剂。我们在体素或区域水平上没有发现两组之间有明显的氟托卡比摄取差异。

结论

在药物水平上使用 MAO-B 抑制剂不会显著影响氟托卡比的结合。因此,MAO-B 似乎不是氟托卡比的一个重要结合靶点。

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