Preliminary PET Study of 18F-FC119S in Normal and Alzheimer's Disease Models

Se Jong Oh; Min Hwan Kim; Sang Jin Han; Kyung Jun Kang; In Ok Ko; Youngsoo Kim; Ji Ae Park; Jae Yong Choi; Kyo Chul Lee; Dae Yoon Chi; Yong Jin Lee; Kyeong Min Kim

doi:10.1021/acs.molpharmaceut.7b00351

Preliminary PET Study of ¹⁸F-FC119S in Normal and Alzheimer's Disease Models

Se Jong Oh, Min Hwan Kim, Sang Jin Han, Kyung Jun Kang, In Ok Ko, Youngsoo Kim, Ji Ae Park, Jae Yong Choi, Kyo Chul Lee, Dae Yoon Chi, Yong Jin Lee, Kyeong Min Kim

Department of Pharmacy

Research output: Contribution to journal › Article › peer-review

9 Citations (Scopus)

Abstract

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.

Original language	English
Pages (from-to)	3114-3120
Number of pages	7
Journal	Molecular Pharmaceutics
Volume	14
Issue number	9
DOIs	https://doi.org/10.1021/acs.molpharmaceut.7b00351
Publication status	Published - 2017 Sept 5

Bibliographical note

Funding 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).

Publisher Copyright:
© 2017 American Chemical Society.

All Science Journal Classification (ASJC) codes

Molecular Medicine
Pharmaceutical Science
Drug Discovery

Access to Document

10.1021/acs.molpharmaceut.7b00351

Cite this

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title = "Preliminary PET Study of 18F-FC119S in Normal and Alzheimer's Disease Models",

abstract = "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.",

author = "Oh, {Se Jong} and Kim, {Min Hwan} and Han, {Sang Jin} and Kang, {Kyung Jun} and Ko, {In Ok} and Youngsoo Kim and Park, {Ji Ae} and Choi, {Jae Yong} and Lee, {Kyo Chul} and Chi, {Dae Yoon} and Lee, {Yong Jin} and Kim, {Kyeong Min}",

note = "Funding 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). Publisher Copyright: {\textcopyright} 2017 American Chemical Society.",

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doi = "10.1021/acs.molpharmaceut.7b00351",

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AU - Oh, Se Jong

AU - Kim, Min Hwan

AU - Han, Sang Jin

AU - Kang, Kyung Jun

AU - Ko, In Ok

AU - Kim, Youngsoo

AU - Park, Ji Ae

AU - Choi, Jae Yong

AU - Lee, Kyo Chul

AU - Chi, Dae Yoon

AU - Lee, Yong Jin

AU - Kim, Kyeong Min

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PY - 2017/9/5

Y1 - 2017/9/5

N2 - 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.

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