Whole-Body Biodistribution and Radiation Dosimetry of 18F-FP-(+)-DTBZ (18F-AV-133): A Novel Vesicular Monoamine Transporter 2 Imaging Agent
| Autor: | Shiaw-Pyng Wey, Hsiu-Ping Chang, Tzu-Chen Yen, Kun-Ju Lin, Ing-Tsung Hsiao, Chin-Song Lu, Daniel Skovronsky, Yi-Hsin Weng, Mei-Ping Kung |
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| Rok vydání: | 2010 |
| Předmět: |
Male
Fluorine Radioisotopes Biodistribution Drug-Related Side Effects and Adverse Reactions Tetrabenazine Vesicular monoamine transporter 2 Effective dose (radiation) medicine Humans Dosimetry Radiology Nuclear Medicine and imaging Large intestine Radiometry medicine.diagnostic_test biology business.industry Equivalent dose Parkinson Disease Middle Aged Imaging agent Molecular Imaging medicine.anatomical_structure Positron emission tomography Positron-Emission Tomography Vesicular Monoamine Transport Proteins biology.protein Female Nuclear medicine business |
| Zdroj: | Journal of Nuclear Medicine. 51:1480-1485 |
| ISSN: | 2159-662X 0161-5505 |
| DOI: | 10.2967/jnumed.110.078196 |
| Popis: | Vesicular monoamine transporter 2 (VMAT2) is highly expressed in the endocrine cells and brain. We investigated the biodistribution and radiation dosimetry of (2R,3R,11bR)-9-(3-(18)F-fluoropropoxy)-3-isobutyl-10-methoxy-2,3,4,6,7,11b-hexahydro-1H-pyrido[2,1-a]isoquinolin-2-ol ((18)F-FP-(+)-dihydrotetrabenazine [DTBZ] or (18)F-AV-133), a potential VMAT2 imaging agent showing encouraging results in humans, to facilitate its future clinical use.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 (18)F-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.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 microGy/MBq, was the pancreas. The effective dose equivalent and effective dose for (18)F-AV-133 were 36.5 +/- 2.8 and 27.8 +/- 2.5 microSv/MBq, respectively. These values are comparable to those reported for any other (18)F-labeled radiopharmaceutical.(18)F-AV-133 is safe, with appropriate biodistribution and radiation dosimetry for imaging VMAT2 sites in humans. |
| Databáze: | OpenAIRE |
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