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. 2017 Apr 21;17(1):27.
doi: 10.1186/s12880-017-0200-1.

Semi-automatic synthesis and biodistribution of N-(2-18F-fluoropropionyl)-bis(zinc (II)-dipicolylamine) (18F-FP-DPAZn2) for AD model imaging

Fuhua Wen  1 , Dahong Nie  1 , Kongzhen Hu  1 , Ganghua Tang  2 , Shaobo Yao  1 , Caihua Tang  1
Affiliations

Semi-automatic synthesis and biodistribution of N-(2-18F-fluoropropionyl)-bis(zinc (II)-dipicolylamine) (18F-FP-DPAZn2) for AD model imaging

Fuhua Wen et al. BMC Med Imaging. .

Abstract

Background: Phosphatidylserine (PS)-targeting positron emission tomography (PET) imaging with labeled small-molecule tracer is a crucial non-invasive molecule imaging method of apoptosis. In this study, semi-automatic radiosynthesis and biodistribution of N-(2-18F-fluoropropionyl)-bis(zinc(II)-dipicolylamine) (18F-FP-DPAZn2), as a potential small-molecule tracer for PET imaging of cell death in Alzheimer's disease (AD) model, were performed.

Methods: 18F-FP-DPAZn2 was synthesized on the modified PET-MF-2V-IT-I synthesizer. Biodistribution was determined in normal mice and PET images of AD model were obtained on a micro PET-CT scanner.

Results: With the modified synthesizer, the total decay-corrected radiochemical yield of 18F-FP-DPAZn2 was 35 ± 6% (n = 5) from 18F- within 105 ± 10 min. Biodistribution results showed that kidney has the highest uptake of 18F-FP-DPAZn2. The uptake of radioactivity in brain kept at a relatively low level during the whole observed time. In vivo 18F-FP-DPAZn2 PET images demonstrated more accumulation of radioactivity in the brain of AD model mice than that in the brain of normal mice.

Conclusions: The semi-automatic synthetic method provides a slightly higher radiochemical yield and shorter whole synthesis time of 18F-FP-DPAZn2 than the manual operation method. This improved method can give enough radioactivity and high radiochemical purity of 18F-FP-DPAZn2 for in vivo PET imaging. The results show that 18F-FP-DPAZn2 seems to be a potential cell death tracer for AD imaging.

Keywords: 18F-FP-DPAZn2; 18F-NFP; Cell death; Semi-automatic synthesis; Zinc(II)-dipicolylamine.

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Figures

Fig. 1
Fig. 1
Schematic diagram of PET-MF-2V-IT-1 synthesis module
Fig. 2
Fig. 2
The radiosynthesis route of 18F-NFP and 18F-FP-DPAZn2
Fig. 3
Fig. 3
HPLC analysis of purified 18F-FP-DPA2 solution coinjected with the standard FP-DPA2. a Radioactive chromatogram; b UV chromatogram at 254 nm
Fig. 4
Fig. 4
The biodistributions of 18F-FP-DPAZn2 (a) and 18F-FB-DPAZn2 (b) in normal mice
Fig. 5
Fig. 5
β-amyloid (Aβ) immunohistochemistry of double transgenic AD models
Fig. 6
Fig. 6
Decay-corrected axial, coronal and sagittal 18F-FP-DPAZn2 PET images of AD model mice and normal mice
See this image and copyright information in PMC

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