To evaluate the efficacy of 18F-FC119S as a positron emission tomography (PET) radiopharmaceutical for the imaging of Alzheimer's disease (AD), we studied the drug absorption characteristics and distribution of 18F-FC119S in normal mice. In addition, we evaluated the specificity of 18F-FC119S for β-amyloid (Aβ) in the AD group of an APP/PS1 mouse model and compared it with that in the wild-type (WT) group. The behavior of 18F-FC119S in the normal mice was characteristic of rapid brain uptake and washout patterns. In most organs, including the brain, 18F-FC119S reached its maximum concentration within 1 min and was excreted via the intestine. Brain PET imaging of 18F-FC119S showed highly specific binding of the molecule to Aβ in the cortex and hippocampus. The brain uptake and binding values for the AD group were higher than those for the WT group. These results indicated that 18F-FC119S would be a candidate PET imaging agent for targeting Aβ plaque.
Bibliographical noteFunding Information:
FutureChem (Korea) is acknowledged for the synthesis of 18F-FC119S. This research was supported by a grant of the Korea Institute of Radiological and Medical Sciences (KIRAMS) funded by the Ministry of Science, ICT & Future Planning, Republic of Korea (No. 1711045578; 1711045556; 1711045577; 1711045576/50532-2017, 1711045539; 171104541/50461-2017).
© 2017 American Chemical Society.
All Science Journal Classification (ASJC) codes
- Molecular Medicine
- Pharmaceutical Science
- Drug Discovery