18F-PBR06 PET/CT imaging for evaluating atherosclerotic plaques linked to macrophage infiltration

The present study explored the 18 kDa translocator protein radioligand [F]N-fluoroacetyl-N-(2,5-dimethoxybenzyl)-2-phenoxyaniline (F-PBR06) targeting macrophages for PET imaging of atherosclerotic plaques and evaluating the vulnerability of atherosclerotic plaques toward rupture.

F-PBR06 was synthesized using a Synthra RNplus module automatically. RAW264.7 cells were used for cell binding study with F-PBR06. In-vivo micro-PET/CT imaging for ApoE mice and C57 mice was performed 1 h after injection of F-PBR06. CD68 and F480 immunofluorescence stainings were performed in the aorta tissues.

In-vitro cell studies showed uptake of F-PBR06 to RAW264.7 cells. Micro-PET/CT imaging identified the atherosclerotic lesions in the aortic arch of ApoE mice successfully, whereas no signal was observed in C57 mice. The ratio of plaque-to-muscle in ApoE mice of 32 weeks was significantly higher than that in ApoE mice of 22 weeks, which was confirmed by CD68 immunofluorescence staining and F480 immunofluorescence staining.

TSPO radioligand F-PBR06 allows noninvasive PET/CT imaging of macrophage-abundant atherosclerotic plaques as well as positive correlation between PET imagings and ex-vivo immunofluorescence staining of plaques in mice with different ages, thereby representing a potential attractive tool for evaluating the vulnerability of atherosclerotic plaques towards rupture.