title: [(18)F]FPEB and [(18)F]FDEGPECO comparative study of mGlu5 quantification in rodent brain.
abstract: The aim of this study is to compare [(18)F]FPEB and [(18)F]FDEGPECO for the quantification of mGlu5 receptors in rodent brains. After preparation of radioligands, dynamic PET data was acquired for 90min. Estimated non-displaceable binding potential (BPND) values were calculated from the non-invasive Logan's graphical analysis method. Although both radioligands showed similar radiochemical amenability, [(18)F]FPEB PET showed higher brain uptake and superior binding potential values than those of [(18)F]FDEGPECO PET (peak brain uptakes in the hippocampus and the striatum: 7.2-8.7 vs. 5.0-6.2, BPND: 7.3-9.6 vs. 0.3-0.4 for [(18)F]FPEB and [(18)F]FDEGPECO, respectively). In addition, the target-to-reference ratios for [(18)F]FPEB is >4 fold than those of [(18)F]FDEGPECO. From this evidence, we conclude that [(18)F]FPEB is a superior radioligand for mGlu5 imaging in preclinical studies.
authors: Department of Biology, Swarthmore College, 500 College Avenue Swarthmore, PA 19081, USA.
authors: Jee Hae
authors: JH
authors: Kang
authors: Department of Nuclear Medicine, Inha University Hospital, Incheon, Republic of Korea.
authors: Minkyung
authors: M
authors: Lee
authors: Department of Nuclear Medicine, Gangnam Severance Hospital, Yonsei University College of Medicine, Seoul, Republic of Korea.
authors: Young Hoon
authors: YH
authors: Ryu
authors: Department of Neurology, Gangnam Severance Hospital, Yonsei University College of Medicine, Seoul, Republic of Korea.
authors: Chul Hyoung
authors: CH
authors: Lyoo
authors: Department of Pharmacology, Yonsei University College of Medicine, Seoul, Republic of Korea; Brain Korea 21 Plus Project for Medical Science, Yonsei University College of Medicine, Seoul, Republic of Korea.
authors: Chul Hoon
authors: CH
authors: Kim
authors: Molecular Imaging Research Center, Korea Institute of Radiological and Medical Sciences, Seoul, Republic of Korea.
authors: Kyo Chul
authors: KC
authors: Lee
authors: Molecular Imaging Research Center, Korea Institute of Radiological and Medical Sciences, Seoul, Republic of Korea.
authors: Tae Hyun
authors: TH
authors: Choi
authors: Department of Nuclear Medicine, Gangnam Severance Hospital, Yonsei University College of Medicine, Seoul, Republic of Korea. Electronic address: smhany@yuhs.ac.
authors: Jae Yong
authors: JY
authors: Choi
mesh_terms: D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism*; D003342:Corpus Striatum / Q000000981:diagnostic imaging / Q000378:metabolism; D005462:Fluorine Radioisotopes; D006624:Hippocampus / Q000000981:diagnostic imaging / Q000378:metabolism; D008297:Male; D009570:Nitriles; D010091:Oximes; D049268:Positron-Emission Tomography / Q000379:methods; D011725:Pyridines; D019275:Radiopharmaceuticals; D051381:Rats; D017207:Rats, Sprague-Dawley; D064529:Receptor, Metabotropic Glutamate 5 / Q000378:metabolism*; D014018:Tissue Distribution
chemical_list: C550155:3-(pyridin-2-ylethynyl)cyclohex-2-enone-O-2-(2-fluoroethoxy)ethyloxime; C527000:3-fluoro-5-((pyridin-3-yl)ethynyl)benzonitrile; D005462:Fluorine Radioisotopes; C578937:Grm5 protein, rat; D009570:Nitriles; D010091:Oximes; D011725:Pyridines; D019275:Radiopharmaceuticals; D064529:Receptor, Metabotropic Glutamate 5
keywords: PET; [(18)F]FDEGPECO; [(18)F]FPEB; mGlu5