Synthesis and preliminary evaluation of [18F]FEtP4A,a promising PET tracer for mapping acetylcholinesterase in vivo |
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Authors: | Zhang Ming-Rong Tsuchiyama Akio Haradahira Terushi Furutsuka Kenji Yoshida Yuichiro Kida Takayo Noguchi Junko Irie Toshiaki Suzuki Kazutoshi |
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Affiliation: | Department of Medical Imaging, National Institute of Radiological Sciences, Chiba, Japan. |
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Abstract: | N-[18F]Fluoroethyl-4-piperidyl acetate ([18F]FEtP4A), an analog of [11C]MP4A for mapping brain acetylcholineseterase (AchE) activity, was prepared by reacting 4-piperidyl acetate (P4A) with [18F]fluoroethyl bromide ([18F]FEtBr) using a newly developed automated system. Preliminary evaluation showed that the initial uptake of [18F]FEtP4A in the mouse brain was > 8% injected dose/g tissue. The distribution pattern of [18F]FEtP4A in the brain was striatum>cerebral cortex>cerebellum within 10-120 min post-injection, which reflected the distribution rank pattern of AchE activity in the brain. Moreover, chemical analysis of in vivo radioactive metabolites in the mouse brain indicated that 83% of [18F]FEtP4A was hydrolyzed to N-[18F]fluoroethyl-4-piperidinol ([18F]FEtP4OH) after 1 min intravenous injection. From these results, [18F]FEtP4A may become a promising PET tracer for mapping the AchE in vivo. |
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