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• W2026791424 abstract "Vesicular monoamine transporter 2 (VMAT2) is highly expressed in the endocrine cells and brain. We investigated the biodistribution and radiation dosimetry of (2<i>R</i>,3<i>R</i>,11b<i>R</i>)-9-(3-¹⁸F-fluoropropoxy)-3-isobutyl-10-methoxy-2,3,4,6,7,11b-hexahydro-1<i>H</i>-pyrido[2,1-<i>a</i>]isoquinolin-2-ol (¹⁸F-FP-(+)-dihydrotetrabenazine [DTBZ] or ¹⁸F-AV-133), a potential VMAT2 imaging agent showing encouraging results in humans, to facilitate its future clinical use. <b>Methods:</b> Nine healthy human subjects (mean age ± SD, 58.6 ± 4.2 y) were enrolled for the whole-body PET scan. Serial images were acquired for 3 h immediately after a bolus injection of 390.7 ± 22.9 MBq of ¹⁸F-AV-133 per individual. The source organs were delineated on PET/CT images. The OLINDA/EXM application was used to determine the equivalent dose for individual organs. <b>Results:</b> The radiotracer did not show any noticeable adverse effects for the 9 subjects examined. The radioactivity uptake in the brain was the highest at 7.5% ± 0.6% injected dose at 10 min after injection. High absorbed doses were found in the pancreas, liver, and upper large intestine wall. The highest-dosed organ, which received 153.3 ± 23.8 μGy/MBq, was the pancreas. The effective dose equivalent and effective dose for ¹⁸F-AV-133 were 36.5 ± 2.8 and 27.8 ± 2.5 μSv/MBq, respectively. These values are comparable to those reported for any other ¹⁸F-labeled radiopharmaceutical. <b>Conclusion:</b>¹⁸F-AV-133 is safe, with appropriate biodistribution and radiation dosimetry for imaging VMAT2 sites in humans." @default.
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• W2026791424 date "2010-08-18" @default.
• W2026791424 modified "2023-09-24" @default.
• W2026791424 title "Whole-Body Biodistribution and Radiation Dosimetry of ¹⁸F-FP-(+)-DTBZ (¹⁸F-AV-133): A Novel Vesicular Monoamine Transporter 2 Imaging Agent" @default.
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• W2026791424 doi "https://doi.org/10.2967/jnumed.110.078196" @default.
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