Tsukuba Research Laboratory, Central Research Laboratory, Hamamatsu Photonics K.K., 5-9-2 Tokodai, Tsukuba, Ibaraki 300-2635, Japan.
PET Research Group, Central Research Laboratory, Hamamatsu Photonics K.K., 5000 Hirakuchi, Hamakita, Hamamatsu, Shizuoka 434-8601, Japan.
Mitochondrion. 2019 May;46:97-102. doi: 10.1016/j.mito.2018.03.001. Epub 2018 Mar 18.
BCPP compounds have been developed as PET imaging probes for neurodegenerative diseases in the living brain. F-BCPP-EF identifies damaged neuronal areas based on the lack of MC-I; however, its underlying mechanisms of action and specificity for MC-I remain unclear. We herein report the effects of BCPP-BF, -EF, -EM on MC-I in respiratory chain complexes using cardiomyocyte SMP. BCPP compounds inhibited the binding of H-dihydrorotenone to MC-I and the proton pumping activity of MC-I in a concentration-dependent manner in vitro. These results suggest that BCPP compounds are MC-I selective inhibitors, and, thus, these radiolabeled compounds are useful for the quantitative imaging of MC-I using PET.
BCPP 化合物已被开发为活体大脑中神经退行性疾病的 PET 成像探针。F-BCPP-EF 基于缺乏 MC-I 来识别受损的神经元区域；然而，其作用机制和对 MC-I 的特异性尚不清楚。我们在此报告了 BCPP-BF、-EF、-EM 对心肌细胞 SMP 中 MC-I 呼吸链复合物的影响。BCPP 化合物在体外以浓度依赖的方式抑制 H-二氢鱼藤酮与 MC-I 的结合以及 MC-I 的质子泵活性。这些结果表明，BCPP 化合物是 MC-I 选择性抑制剂，因此，这些放射性标记化合物可用于使用 PET 对 MC-I 进行定量成像。
