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

 Talakad G Lohith  ;  Tetsuya Tsujikawa  ;  Fabrice G Sime´on  ;  Mattia Veronese  ;  Sami S Zoghbi  ;  Chul Hyoung Lyoo  ;  Yasuyuki Kimura  ;  Cheryl L Morse  ;  Victor W Pike  ;  Masahiro Fujita  ;  Robert B Innis 
 Journal of Cerebral Blood Flow and Metabolism, Vol.37(7) : 2458-2470, 2017 
Journal Title
 Journal of Cerebral Blood Flow and Metabolism 
Issue Date
Adult ; Brain/diagnostic imaging* ; Brain/metabolism* ; Carbon Radioisotopes ; Female ; Healthy Volunteers ; Humans ; Image Processing, Computer-Assisted ; Ligands ; Male ; Models, Biological ; Nitriles/blood ; Nitriles/pharmacokinetics* ; Positron-Emission Tomography/methods* ; Pyridines/blood ; Pyridines/pharmacokinetics* ; RNA, Messenger/genetics ; Radionuclide Imaging ; Radiopharmaceuticals/pharmacokinetics ; Receptor, Metabotropic Glutamate 5/genetics ; Receptor, Metabotropic Glutamate 5/metabolism* ; Thiazoles/blood ; Thiazoles/pharmacokinetics* ; Tissue Distribution ; Whole Body Imaging
FPEB ; PET imaging ; SP203 ; genomic plot ; mGluR5
Of the two 18F-labeled PET ligands currently available to image metabotropic glutamate receptor 5 (mGluR5), [18F]FPEB is reportedly superior because [18F]SP203 undergoes glutathionlyation, generating [18F]-fluoride ion that accumulates in brain and skull. To allow multiple PET studies on the same day with lower radiation exposure, we prepared [11C]FPEB and [11C]SP203 from [11C]hydrogen cyanide and compared their abilities to accurately quantify mGluR5 in human brain, especially as regards radiometabolite accumulation. Genomic plot was used to estimate the ratio of specific-to-nondisplaceable uptake ( BPND) without using a receptor blocking drug. Both tracers quantified mGluR5; however [11C]SP203, like [18F]SP203, had radiometabolite accumulation in brain, as evidenced by increased distribution volume ( VT) over the scan period. Absolute VT values were ∼30% lower for 11C-labeled compared with 18F-labeled radioligands, likely caused by the lower specific activities (and high receptor occupancies) of the 11C radioligands. The genomic plot indicated ∼60% specific binding in cerebellum, which makes it inappropriate as a reference region. Whole-body scans performed in healthy subjects demonstrated a low radiation burden typical for 11C-ligands. Thus, the evidence suggests that [11C]FPEB is superior to [11C]SP203. If prepared in higher specific activity, [11C]FPEB would presumably be as effective as [18F]FPEB for quantifying mGluR5 in human brain.
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1. College of Medicine (의과대학) > Dept. of Neurology (신경과학교실) > 1. Journal Papers
Yonsei Authors
Lyoo, Chul Hyoung(류철형) ORCID logo https://orcid.org/0000-0003-2231-672X
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