Literature DB >> 22895910

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

Romina Mizrahi1, Pablo M Rusjan, Irina Vitcu, Alvina Ng, Alan A Wilson, Sylvain Houle, Peter M Bloomfield.   

Abstract

PURPOSE: [(18)F]-FEPPA is a translocator protein (18 kDa, TSPO) positron emission tomography (PET) radiotracer. Radiation dosimetry was estimated from the whole body biodistribution, taking into consideration TSPO rs6971 (Ala147Thr) polymorphism. PROCEDURES: [(18)F]-FEPPA whole body PET scans were acquired for six healthy subjects. Time-activity curves were generated from regions of interest of nine organs, from which normalized accumulated activities were calculated and thus internal dose, using OLINDA/EXM 1.1. Genotyping of rs6971, associated with high- and low-affinity [(18)F]-FEPPA binding (high-affinity binder (HAB) and low-affinity binder (LAB)), was performed.
RESULTS: Five subjects exhibited the C/C (HAB) allele, and the other carried the minor allele T/T (LAB). The LAB whole body biodistribution showed highest radioactivity accumulation in bladder, whereas in HABs, the spleen received the highest dose. The effective dose of the single LAB (16.3 μSv/MBq) was 23 % less than the mean of the HABs (21.0 ± 2.9 μSv/MBq). When including all subjects, the effective dose was 20.2 ± 3.0 μSv/MBq.
CONCLUSIONS: [(18)F]-FEPPA radiation dose is consistent with other (18)F-labeled radioligands and the Ala147Thr genotype agreed with [(18)F]-FEPPA distribution.

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Year:  2013        PMID: 22895910     DOI: 10.1007/s11307-012-0589-4

Source DB:  PubMed          Journal:  Mol Imaging Biol        ISSN: 1536-1632            Impact factor:   3.488


  35 in total

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Authors:  Marco Brambilla; Chiara Secco; Marco Dominietto; Roberta Matheoud; Gianmauro Sacchetti; Eugenio Inglese
Journal:  J Nucl Med       Date:  2005-12       Impact factor: 10.057

2.  High densities of benzodiazepine receptors in human cortical areas.

Authors:  C Braestrup; R Albrechtsen; R F Squires
Journal:  Nature       Date:  1977-10-20       Impact factor: 49.962

3.  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

4.  In vivo visualization of activated glia by [11C] (R)-PK11195-PET following herpes encephalitis reveals projected neuronal damage beyond the primary focal lesion.

Authors:  A Cagnin; R Myers; R N Gunn; A D Lawrence; T Stevens; G W Kreutzberg; T Jones; R B Banati
Journal:  Brain       Date:  2001-10       Impact factor: 13.501

5.  In vivo imaging of activated microglia using [11C]PK11195 and positron emission tomography in patients after ischemic stroke.

Authors:  A Gerhard; B Neumaier; E Elitok; G Glatting; V Ries; R Tomczak; A C Ludolph; S N Reske
Journal:  Neuroreport       Date:  2000-09-11       Impact factor: 1.837

Review 6.  The peripheral benzodiazepine receptor (Translocator protein 18kDa) in microglia: from pathology to imaging.

Authors:  Sriram Venneti; Brian J Lopresti; Clayton A Wiley
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7.  Biodistribution and radiation dosimetry in humans of a new PET ligand, (18)F-PBR06, to image translocator protein (18 kDa).

Authors:  Yota Fujimura; Yasuyuki Kimura; Fabrice G Siméon; Leah P Dickstein; Victor W Pike; Robert B Innis; Masahiro Fujita
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8.  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

9.  Design, synthesis, and structure-activity relationships of novel tetracyclic compounds as peripheral benzodiazepine receptor ligands.

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10.  Increased binding of peripheral benzodiazepine receptor in Alzheimer's disease measured by positron emission tomography with [11C]DAA1106.

Authors:  Fumihiko Yasuno; Miho Ota; Jun Kosaka; Hiroshi Ito; Makoto Higuchi; Talant K Doronbekov; Shoko Nozaki; Yota Fujimura; Michihiko Koeda; Takashi Asada; Tetsuya Suhara
Journal:  Biol Psychiatry       Date:  2008-06-02       Impact factor: 13.382

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Authors:  Victor W Pike
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2.  Biodistribution and Radiation Dosimetry for the Novel SV2A Radiotracer [(18)F]UCB-H: First-in-Human Study.

Authors:  F Bretin; M A Bahri; C Bernard; G Warnock; J Aerts; N Mestdagh; T Buchanan; C Otoul; F Koestler; F Mievis; F Giacomelli; C Degueldre; R Hustinx; A Luxen; A Seret; A Plenevaux; E Salmon
Journal:  Mol Imaging Biol       Date:  2015-08       Impact factor: 3.488

Review 3.  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
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4.  Influence of TSPO genotype on 11C-PBR28 standardized uptake values.

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Journal:  J Nucl Med       Date:  2013-06-19       Impact factor: 10.057

Review 5.  Mapping neuroinflammation in frontotemporal dementia with molecular PET imaging.

Authors:  Jing Zhang
Journal:  J Neuroinflammation       Date:  2015-05-29       Impact factor: 8.322

6.  Imaging adipose tissue browning using the TSPO-18kDa tracer [18F]FEPPA.

Authors:  S V Hartimath; S Khanapur; R Boominathan; L Jiang; P Cheng; F F Yong; P W Tan; E G Robins; J L Goggi
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7.  GMP-compliant fully automated radiosynthesis of [18F]FEPPA for PET/MRI imaging of regional brain TSPO expression.

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8.  Neuroinflammation in Low-Level PM2.5-Exposed Rats Illustrated by PET via an Improved Automated Produced [18F]FEPPA: A Feasibility Study.

Authors:  Mei-Fang Cheng; Tsun-Jen Cheng; Yue Leon Guo; Ching-Hung Chiu; Hung-Ming Wu; Ruoh-Fang Yen; Ya-Yao Huang; Wen-Sheng Huang; Chyng-Yann Shiue
Journal:  Mol Imaging       Date:  2022-06-07       Impact factor: 3.250

9.  An Optimized MicroPET Imaging Method for the Distribution and Synergies of Natural Products.

Authors:  Qingxin Cui; Yang Liu; Mengge Zhou; Yanqi Han; Chengcheng Yin; Gang Bai
Journal:  Front Pharmacol       Date:  2018-08-21       Impact factor: 5.810

10.  [18F]FEPPA PET imaging for monitoring CD68-positive microglia/macrophage neuroinflammation in nonhuman primates.

Authors:  Matthew Zammit; Yunlong Tao; Miles E Olsen; Jeanette Metzger; Scott C Vermilyea; Kathryn Bjornson; Maxim Slesarev; Walter F Block; Kerri Fuchs; Sean Phillips; Viktorya Bondarenko; Su-Chun Zhang; Marina E Emborg; Bradley T Christian
Journal:  EJNMMI Res       Date:  2020-08-06       Impact factor: 3.138

  10 in total

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