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Synthesis and in vitro cellular uptake of 11C-labeled 5-aminolevulinic acid derivative to estimate the induced cellular accumulation of protoporphyrin IX |
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| Authors: | Chie Suzuki Koichi Kato Atsushi B Tsuji Tatsuya Kikuchi Ming-Rong Zhang Yasushi Arano Tsuneo Saga |
| Institution: | 1. Diagnostic Imaging Group, Molecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan;2. Department of Molecular Imaging and Radiotherapy, Graduate School of Pharmaceutical Sciences, Chiba University, 1-8-1 Inohana, Chuo-ku, Chiba 260-8675, Japan;3. Department of Integrative Brain Imaging, National Center of Neurology and Psychiatry, 4-1-1 Ogawahigashi-cho, Kodaira, Tokyo 187-5551, Japan;4. Molecular Probe Group, Molecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan |
| Abstract: | Protoporphyrin IX (PpIX) accumulation induced by exogenous 5-aminolevulinic acid (ALA) in tumors affects the therapeutic efficacy of ALA-based photodynamic and sonodynamic therapies. To develop a new imaging probe to estimate the ALA-induced PpIX accumulation, 11C-labeled ALA analog (4), an ALA-dehydratase inhibitor, was radiosynthesized via 11C-methylation of a Schiff-base-activated precursor in the presence of tetrabutylammonium fluoride, followed by the hydrolysis of ester and imine groups. The cellular uptake of 4 linearly increased with time and was inhibited by ALA and other transporter competitors. Monitoring analog 4 with positron emission tomography might be useful to estimate the ALA-induced PpIX accumulation in tumors. |
| Keywords: | 5-Aminolevulinic acid (ALA) Photodynamic therapy (PDT) Sonodynamic therapy (SDT) Positron emission tomography (PET) Radiosynthesis |
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