Literature DB >> 20585776

Biodistribution and radiation dosimetry of a positron emission tomographic ligand, 18F-SP203, to image metabotropic glutamate subtype 5 receptors in humans.

Yasuyuki Kimura1, Fabrice G Siméon, Jun Hatazawa, P David Mozley, Victor W Pike, Robert B Innis, Masahiro Fujita.   

Abstract

PURPOSE: A new PET ligand, 3-fluoro-5-(2-(2-(18)F-(fluoromethyl)-thiazol-4-yl)ethynyl)benzonitrile ((18)F-SP203), is a positron emission tomographic radioligand selective for metabotropic glutamate subtype 5 receptors. The purposes of this study were to estimate the radiation-absorbed doses of (18)F-SP203 in humans and to determine from the distribution of radioactivity in bone structures with various proportions of bone and red marrow whether (18)F-SP203 undergoes defluorination.
METHODS: Whole-body images were acquired for 5 h after injecting (18)F-SP203 in seven healthy humans. Urine was collected at various time points. Radiation-absorbed doses were estimated by the Medical Internal Radiation Dose scheme.
RESULTS: After injecting (18)F-SP203, the two organs with highest radiation exposure were urinary bladder wall and gallbladder wall, consistent with both urinary and fecal excretion. In the skeleton, most of the radioactivity was in bone structures that contain red marrow and not in those without red marrow. Although the dose to red marrow (30.9 microSv/MBq) was unusually high, the effective dose (17.8 microSv/MBq) of (18)F-SP203 was typical of that of other (18)F radiotracers.
CONCLUSION: (18)F-SP203 causes an effective dose in humans typical of several other (18)F radioligands and undergoes little defluorination.

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Year:  2010        PMID: 20585776      PMCID: PMC3207261          DOI: 10.1007/s00259-010-1447-8

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


  23 in total

1.  Human biodistribution and radiation dosimetry of the tachykinin NK1 antagonist radioligand [18F]SPA-RQ: comparison of thin-slice, bisected, and 2-dimensional planar image analysis.

Authors:  David R Sprague; Frederick T Chin; Jeih-San Liow; Masahiro Fujita; H Donald Burns; Richard Hargreaves; James B Stubbs; Victor W Pike; Robert B Innis; P David Mozley
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2.  Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography.

Authors:  Fabrice G Siméon; Amira K Brown; Sami S Zoghbi; Velvet M Patterson; Robert B Innis; Victor W Pike
Journal:  J Med Chem       Date:  2007-06-16       Impact factor: 7.446

3.  Radiodefluorination of 3-fluoro-5-(2-(2-[18F](fluoromethyl)-thiazol-4-yl)ethynyl)benzonitrile ([18F]SP203), a radioligand for imaging brain metabotropic glutamate subtype-5 receptors with positron emission tomography, occurs by glutathionylation in rat brain.

Authors:  H Umesha Shetty; Sami S Zoghbi; Fabrice G Siméon; Jeih-San Liow; Amira K Brown; Pavitra Kannan; Robert B Innis; Victor W Pike
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5.  Synthesis, characterization, and first successful monkey imaging studies of metabotropic glutamate receptor subtype 5 (mGluR5) PET radiotracers.

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7.  Radiosynthesis and preclinical evaluation of 11C-ABP688 as a probe for imaging the metabotropic glutamate receptor subtype 5.

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Authors:  Simon M Ametamey; Valerie Treyer; Johannes Streffer; Matthias T Wyss; Mark Schmidt; Milen Blagoev; Samuel Hintermann; Yves Auberson; Fabrizio Gasparini; Uta C Fischer; Alfred Buck
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9.  Disulfiram inhibits defluorination of (18)F-FCWAY, reduces bone radioactivity, and enhances visualization of radioligand binding to serotonin 5-HT1A receptors in human brain.

Authors:  Yong Hoon Ryu; Jeih-San Liow; Sami Zoghbi; Masahiro Fujita; Jerry Collins; Dnyanesh Tipre; Janet Sangare; Jinsoo Hong; Victor W Pike; Robert B Innis
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10.  Metabotropic glutamate subtype 5 receptors are quantified in the human brain with a novel radioligand for PET.

Authors:  Amira K Brown; Yasuyuki Kimura; Sami S Zoghbi; Fabrice G Siméon; Jeih-San Liow; William C Kreisl; Andrew Taku; Masahiro Fujita; Victor W Pike; Robert B Innis
Journal:  J Nucl Med       Date:  2008-12       Impact factor: 10.057

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5.  Synthesis and characterization in monkey of [11C]SP203 as a radioligand for imaging brain metabotropic glutamate 5 receptors.

Authors:  Fabrice G Siméon; Jeih-San Liow; Yi Zhang; Jinsoo Hong; Robert L Gladding; Sami S Zoghbi; Robert B Innis; Victor W Pike
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Authors:  Rajapillai L I Pillai; Dnyanesh N Tipre
Journal:  Eur J Nucl Med Mol Imaging       Date:  2016-01-07       Impact factor: 9.236

7.  Development of [(123)I]IPEB and [(123)I]IMPEB as SPECT Radioligands for Metabotropic Glutamate Receptor Subtype 5.

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8.  Comparison of two PET radioligands, [11C]FPEB and [11C]SP203, for quantification of metabotropic glutamate receptor 5 in human brain.

Authors:  Talakad G Lohith; Tetsuya Tsujikawa; Fabrice G Siméon; Mattia Veronese; Sami S Zoghbi; Chul Hyoung Lyoo; Yasuyuki Kimura; Cheryl L Morse; Victor W Pike; Masahiro Fujita; Robert B Innis
Journal:  J Cereb Blood Flow Metab       Date:  2016-01-01       Impact factor: 6.200

9.  Toxicity and radiation dosimetry studies of the serotonin transporter radioligand [(18) F]AFM in rats and monkeys.

Authors:  Ya-Yao Huang; Chen-Yi Cheng; Wen-Sheng Huang; Kuo-Hsing Ma; Ta-Wei Tseng; Ta-Kai Chou; Yiyun Huang; Chyng-Yann Shiue
Journal:  EJNMMI Res       Date:  2014-12-29       Impact factor: 3.138

10.  Evaluation of the biodistribution and radiation dosimetry of the 18F-labelled amyloid imaging probe [18F]FACT in humans.

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Journal:  EJNMMI Res       Date:  2013-04-24       Impact factor: 3.138

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