Literature DB >> 21732107

Biodistribution and radiation dosimetry of the 18 kDa translocator protein (TSPO) radioligand [18F]FEDAA1106: a human whole-body PET study.

Akihiro Takano1, Balázs Gulyás, Andrea Varrone, Per Karlsson, Nils Sjoholm, Stig Larsson, Cathrine Jonsson, Richard Odh, Richard Sparks, Nabil Al Tawil, Anja Hoffmann, Torsten Zimmermann, Andrea Thiele, Christer Halldin.   

Abstract

PURPOSE: [(18)F]FEDAA1106 is a recently developed positron emission tomography (PET) radioligand for in vivo quantification of the 18 kDa translocator protein [TSPO or, as earlier called, the peripheral benzodiazepine receptor (PBR)]. TSPO imaging is expected to be useful for the clinical evaluation of neuroinflammatory diseases. The aim of this study was to provide dosimetry estimates for [(18)F]FEDAA1106 based on human whole-body PET measurements.
METHODS: PET scans were performed for a total of 6.6 h after the injection of 183.8 ± 9.1 MBq of [(18)F]FEDAA1106 in six healthy subjects. Regions of interest were drawn on coronal images. Estimates of the absorbed doses of radiation were calculated using the OLINDA software.
RESULTS: Peak uptake was largest in lungs, followed by liver, small intestine, kidney, spleen and other organs. Peak values of the percent injected dose (%ID) at a time after radioligand injection were calculated for the lungs (27.1%ID at 0.2 h), liver (21.1%ID at 0.6 h), small intestine (10.4%ID at 6.3 h), kidney (4.9%ID at 1.8 h) and spleen (4.6%ID at 0.6 h). The largest absorbed dose was found in the spleen (0.12 mSv/MBq), followed by kidneys (0.094 mSv/MBq). The calculated mean effective dose was 0.036 mSv/MBq.
CONCLUSION: Based on the distribution and dose estimates, the estimated radiation burden of [(18)F]FEDAA1106 is moderately higher than that of [(18)F]fluorodeoxyglucose (FDG). In clinical studies, the administered activity of this radioligand ought to be adjusted in line with regional regulations. This result would be helpful for further clinical TSPO imaging studies.

Entities:  

Mesh:

Substances:

Year:  2011        PMID: 21732107     DOI: 10.1007/s00259-011-1864-3

Source DB:  PubMed          Journal:  Eur J Nucl Med Mol Imaging        ISSN: 1619-7070            Impact factor:   9.236


  40 in total

1.  Long-term trans-synaptic glial responses in the human thalamus after peripheral nerve injury.

Authors:  R B Banati; A Cagnin; D J Brooks; R N Gunn; R Myers; T Jones; R Birch; P Anand
Journal:  Neuroreport       Date:  2001-11-16       Impact factor: 1.837

2.  Whole-body distribution and metabolism of [N-methyl-11C](R)-1-(2-chlorophenyl)-N-(1-methylpropyl)-3-isoquinolinecarboxamide in humans; an imaging agent for in vivo assessment of peripheral benzodiazepine receptor activity with positron emission tomography.

Authors:  Anne Roivainen; Kjell Någren; Jussi Hirvonen; Vesa Oikonen; Pauliina Virsu; Tuula Tolvanen; Juha O Rinne
Journal:  Eur J Nucl Med Mol Imaging       Date:  2008-12-03       Impact factor: 9.236

3.  Macrophage and astrocyte populations in relation to [3H]PK 11195 binding in rat cerebral cortex following a local ischaemic lesion.

Authors:  R Myers; L G Manjil; B M Cullen; G W Price; R S Frackowiak; J E Cremer
Journal:  J Cereb Blood Flow Metab       Date:  1991-03       Impact factor: 6.200

Review 4.  Basic anatomical and physiological data for use in radiological protection: the skeleton. A report of a Task Group of Committee 2 of the International Commission on Radiological Protection.

Authors: 
Journal:  Ann ICRP       Date:  1995

5.  Quantitative analysis for estimating binding potential of the peripheral benzodiazepine receptor with [(11)C]DAA1106.

Authors:  Yoko Ikoma; Fumihiko Yasuno; Hiroshi Ito; Tetsuya Suhara; Miho Ota; Hinako Toyama; Yota Fujimura; Akihiro Takano; Jun Maeda; Ming-Rong Zhang; Ryuji Nakao; Kazutoshi Suzuki
Journal:  J Cereb Blood Flow Metab       Date:  2006-05-10       Impact factor: 6.200

Review 6.  Translocator protein (18kDa): new nomenclature for the peripheral-type benzodiazepine receptor based on its structure and molecular function.

Authors:  Vassilios Papadopoulos; Mario Baraldi; Tomás R Guilarte; Thomas B Knudsen; Jean-Jacques Lacapère; Peter Lindemann; Michael D Norenberg; David Nutt; Abraham Weizman; Ming-Rong Zhang; Moshe Gavish
Journal:  Trends Pharmacol Sci       Date:  2006-07-05       Impact factor: 14.819

7.  Effects on free radical generation by ligands of the peripheral benzodiazepine receptor in cultured neural cells.

Authors:  A R Jayakumar; K S Panickar; M D Norenberg
Journal:  J Neurochem       Date:  2002-12       Impact factor: 5.372

8.  OLINDA/EXM: the second-generation personal computer software for internal dose assessment in nuclear medicine.

Authors:  Michael G Stabin; Richard B Sparks; Eric Crowe
Journal:  J Nucl Med       Date:  2005-06       Impact factor: 10.057

Review 9.  Multiple forms and locations for the peripheral-type benzodiazepine receptor.

Authors:  M J Woods; D C Williams
Journal:  Biochem Pharmacol       Date:  1996-12-24       Impact factor: 5.858

10.  Human biodistribution and radiation dosimetry of 11C-(R)-PK11195, the prototypic PET ligand to image inflammation.

Authors:  Jussi Hirvonen; Anne Roivainen; Jere Virta; Semi Helin; Kjell Någren; Juha O Rinne
Journal:  Eur J Nucl Med Mol Imaging       Date:  2009-10-28       Impact factor: 9.236

View more
  11 in total

1.  Imaging of neuroinflammation.

Authors:  Andrea Ciarmiello
Journal:  Eur J Nucl Med Mol Imaging       Date:  2011-12       Impact factor: 9.236

2.  Current imaging strategies in rheumatoid arthritis.

Authors:  Merissa N Zeman; Peter Jh Scott
Journal:  Am J Nucl Med Mol Imaging       Date:  2012-03-28

3.  In vivo imaging of the 18-kDa translocator protein (TSPO) with [18F]FEDAA1106 and PET does not show increased binding in Alzheimer's disease patients.

Authors:  Andrea Varrone; Patrik Mattsson; Anton Forsberg; Akihiro Takano; Sangram Nag; Balázs Gulyás; Jacqueline Borg; Ronald Boellaard; Nabil Al-Tawil; Maria Eriksdotter; Torsten Zimmermann; Marcus Schultze-Mosgau; Andrea Thiele; Anja Hoffmann; Adriaan A Lammertsma; Christer Halldin
Journal:  Eur J Nucl Med Mol Imaging       Date:  2013-02-22       Impact factor: 9.236

Review 4.  Considerations in the Development of Reversibly Binding PET Radioligands for Brain Imaging.

Authors:  Victor W Pike
Journal:  Curr Med Chem       Date:  2016       Impact factor: 4.530

5.  Whole body biodistribution and radiation dosimetry in humans of a new PET ligand, [(18)F]-FEPPA, to image translocator protein (18 kDa).

Authors:  Romina Mizrahi; Pablo M Rusjan; Irina Vitcu; Alvina Ng; Alan A Wilson; Sylvain Houle; Peter M Bloomfield
Journal:  Mol Imaging Biol       Date:  2013-06       Impact factor: 3.488

Review 6.  Novel PET Imaging of Inflammatory Targets and Cells for the Diagnosis and Monitoring of Giant Cell Arteritis and Polymyalgia Rheumatica.

Authors:  Kornelis S M van der Geest; Maria Sandovici; Pieter H Nienhuis; Riemer H J A Slart; Peter Heeringa; Elisabeth Brouwer; William F Jiemy
Journal:  Front Med (Lausanne)       Date:  2022-06-06

7.  [18F]FEPPA: Improved Automated Radiosynthesis, Binding Affinity, and Preliminary in Vitro Evaluation in Colorectal Cancer.

Authors:  Neydher Berroterán-Infante; Theresa Balber; Petra Fürlinger; Michael Bergmann; Rupert Lanzenberger; Marcus Hacker; Markus Mitterhauser; Wolfgang Wadsak
Journal:  ACS Med Chem Lett       Date:  2018-02-21       Impact factor: 4.345

8.  Radiation dosimetry of the α4β2 nicotinic receptor ligand (+)-[18F]flubatine, comparing preclinical PET/MRI and PET/CT to first-in-human PET/CT results.

Authors:  Mathias Kranz; Bernhard Sattler; Solveig Tiepolt; Stephan Wilke; Winnie Deuther-Conrad; Cornelius K Donat; Steffen Fischer; Marianne Patt; Andreas Schildan; Jörg Patt; René Smits; Alexander Hoepping; Jörg Steinbach; Osama Sabri; Peter Brust
Journal:  EJNMMI Phys       Date:  2016-10-21

Review 9.  Molecular Imaging of Neuroinflammation in Neurodegenerative Dementias: The Role of In Vivo PET Imaging.

Authors:  Chiara Cerami; Leonardo Iaccarino; Daniela Perani
Journal:  Int J Mol Sci       Date:  2017-05-05       Impact factor: 5.923

10.  In vivo TSPO imaging in patients with multiple sclerosis: a brain PET study with [18F]FEDAA1106.

Authors:  Akihiro Takano; Fredrik Piehl; Jan Hillert; Andrea Varrone; Sangram Nag; Balázs Gulyás; Per Stenkrona; Victor L Villemagne; Christopher C Rowe; Richard Macdonell; Nabil Al Tawil; Thomas Kucinski; Torsten Zimmermann; Marcus Schultze-Mosgau; Andrea Thiele; Anja Hoffmann; Christer Halldin
Journal:  EJNMMI Res       Date:  2013-04-24       Impact factor: 3.138

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.