Kanazawa Masakatsu, Ohba Hiroyuki, Iwazaki Aiko, Kakiuchi Takeharu, Tsukada Hideo
Central Research Laboratory, Hamamatsu Photonics K.K., 5000 Hirakuchi, Hamakita, Hamamatsu, Shizuoka 434-8601, Japan.
Central Research Laboratory, Hamamatsu Photonics K.K., 5000 Hirakuchi, Hamakita, Hamamatsu, Shizuoka 434-8601, Japan.
Bioorg Med Chem. 2015 Feb 15;23(4):729-34. doi: 10.1016/j.bmc.2014.12.061. Epub 2015 Jan 3.
A novel PET probe, 6-[(11)C]methyl-m-tyrosine ([(11)C]6MemTyr), was developed for quantitative imaging of presynaptic dopamine (DA) synthesis in the living brain using positron emission tomography (PET). This probe was evaluated by comparison with conventional 6-[(18)F]fluoro-l-dopa ([(18)F]FDOPA). [(11)C]6MemTyr was labeled using rapid Pd(0)-mediated C-[(11)C]methylation with [(11)C]methyl iodide. The synthesis time was only 35min, and its radiochemical yield was 76%, with radiochemical purity of >99%. PET measurements indicated that [(11)C]6MemTyr could image presynaptic DA synthesis in the striatum of living monkey brain, providing much higher contrast between the striatum and the cerebellum than that with [(18)F]FDOPA.
一种新型正电子发射断层显像（PET）探针6-[(11)C]甲基间酪氨酸（[(11)C]6MemTyr）被开发用于利用正电子发射断层显像（PET）对活体大脑中突触前多巴胺（DA）合成进行定量成像。通过与传统的6-[(18)F]氟-L-多巴（[(18)F]FDOPA）比较对该探针进行了评估。[(11)C]6MemTyr通过使用[(11)C]甲基碘的快速钯（0）介导的C-[(11)C]甲基化进行标记。合成时间仅为35分钟，其放射化学产率为76%，放射化学纯度>99%。PET测量表明，[(11)C]6MemTyr能够对活体猴脑纹状体中的突触前DA合成进行成像，与[(18)F]FDOPA相比，在纹状体和小脑之间提供了更高的对比度。
