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• W2895538433 abstract "6‐[ 18 F]Fluorodopamine ([ 18 F]F‐DA) is taken into cells via the norepinephrine transporter (NET). Recent [ 18 F]F‐DA positron emission tomography–computed tomography (PET‐CT) imaging of adult neuroendocrine tumors shows a dramatic improvement in sensitivity over the standard‐of‐care, meta ‐iodobenzylguanidine (MIBG) single‐photon emission computed tomography (SPECT)–CT. A new precursor (ALPdopamine™) allows no‐carrier‐added synthesis resulting in high–molar activity [ 18 F]F‐DA. Automated synthesis of [ 18 F]F‐DA was performed in a single reactor using a two‐step procedure: 1) fluorination via thermolysis of a diaryliodonium salt precursor, followed by 2) acid hydrolysis. Phase transfer agents, Kryptofix 222 and two tetraalkylammonium salts, were investigated. Optimized synthesis of [ 18 F]F‐DA was achieved in 56 to 60 minutes (26% end of synthesis [EOS], nondecay corrected). The product passed all Food and Drug Administration (FDA)–required quality control testing for human use. Accumulation of [ 18 F]F‐DA in SK‐N‐BE(2)‐C (high NET expression) cells was significantly higher than in SH‐EP (minimal NET expression) cells ( P < 0.0001). ALPdopamine provides an effective scaffold for the routine production of [ 18 F]F‐DA for human use. Validation of uptake by neuroblastoma (NB) cell lines supports the use of [ 18 F]F‐DA for imaging NB patients. A pediatric NB imaging trial using [ 18 F]F‐DA PET has been approved (Investigational New Drug application (IND) no. 138638) based on the methods reported here. We expect [ 18 F]F‐DA will be localized in NB tumors and that high‐quality functional images will be obtained within minutes after injection." @default.
• W2895538433 created "2018-10-12" @default.
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• W2895538433 date "2018-10-22" @default.
• W2895538433 modified "2023-10-17" @default.
• W2895538433 title "Improved, one‐pot synthesis of 6‐[¹⁸F]fluorodopamine and quality control testing for use in patients with neuroblastoma" @default.
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• W2895538433 doi "https://doi.org/10.1002/jlcr.3685" @default.
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