Literature DB >> 12482423

[18F]FMDAA1106 and [18F]FEDAA1106: two positron-emitter labeled ligands for peripheral benzodiazepine receptor (PBR).

Ming Rong Zhang1, Jun Maeda, Kenji Furutsuka, Yuichiro Yoshida, Masanao Ogawa, Tetsuya Suhara, Kazutoshi Suzuki.   

Abstract

We synthesized and evaluated N-(5-fluoro-2-phenoxyphenyl)-N-(2-[(18)F]fluoromethyl-5-methoxybenzyl)acetamide ([(18)F]-FMDAA1106) and N-(5-fluoro-2-phenoxyphenyl)-N-(2-[(18)F]fluoroethyl-5-methoxybenzyl)acetamide ([(18)F]FEDAA1106) as two potent radioligands for peripheral benzodiazepine receptors (PBR). [(18)F]FMDAA1106 and [(18)F]FEDAA1106 were respectively synthesized by fluoroalkylation of the desmethyl precursor DAA1123 with [(18)F]FCH(2)I and [(18)F]FCH(2)CH(2)Br. Ex vivo autoradiograms of [(18)F]FMDAA1106 and [(18)F]FEDAA1106 binding sites in the rat brains revealed that a high radioactivity was present in the olfactory bulb, the highest PBR density region in the brain.

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Year:  2003        PMID： 12482423     DOI： 10.1016/s0960-894x(02)00886-7

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  18 in total

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

Authors:  Akihiro Takano; 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
Journal:  Eur J Nucl Med Mol Imaging       Date:  2011-07-06       Impact factor: 9.236

2.  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 3.  Sifting through the surfeit of neuroinflammation tracers.

Authors:  Paul Cumming; Bjorn Burgher; Omkar Patkar; Michael Breakspear; Neil Vasdev; Paul Thomas; Guo-Jun Liu; Richard Banati
Journal:  J Cereb Blood Flow Metab       Date:  2017-12-19       Impact factor: 6.200

4.  Radiosynthesis and evaluation of 4-(6-[18F]Fluoro-4-(5-isopropoxy-1H-indazol-3-yl)pyridin-2-yl)morpholine as a novel radiotracer candidate targeting leucine-rich repeat kinase 2.

Authors:  Wakana Mori; Tomoteru Yamasaki; Yasushi Hattori; Yiding Zhang; Katsushi Kumata; Masayuki Fujinaga; Masayuki Hanyu; Nobuki Nengaki; Hong Zhang; Ming-Rong Zhang
Journal:  RSC Med Chem       Date:  2020-05-19

Review 5.  Nuclear imaging of neuroinflammation: a comprehensive review of [11C]PK11195 challengers.

Authors:  Fabien Chauveau; Hervé Boutin; Nadja Van Camp; Frédéric Dollé; Bertrand Tavitian
Journal:  Eur J Nucl Med Mol Imaging       Date:  2008-10-01       Impact factor: 9.236

6.  Single-step high-yield radiosynthesis and evaluation of a sensitive 18F-labeled ligand for imaging brain peripheral benzodiazepine receptors with PET.

Authors:  Emmanuelle Briard; Sami S Zoghbi; Fabrice G Siméon; Masao Imaizumi; Jonathan P Gourley; H Umesha Shetty; Shuiyu Lu; Masahiro Fujita; Robert B Innis; Victor W Pike
Journal:  J Med Chem       Date:  2009-02-12       Impact factor: 7.446

Review 7.  Recent Progress in the Development of TSPO PET Ligands for Neuroinflammation Imaging in Neurological Diseases.

Authors:  Md Maqusood Alam; Jihye Lee; Sang-Yoon Lee
Journal:  Nucl Med Mol Imaging       Date:  2017-03-16

8.  Pharmacological evaluation of [123I]-CLINDE: a radioiodinated imidazopyridine-3-acetamide for the study of peripheral benzodiazepine binding sites (PBBS).

Authors:  Filomena Mattner; Karine Mardon; Andrew Katsifis
Journal:  Eur J Nucl Med Mol Imaging       Date:  2007-12-05       Impact factor: 9.236

9.  Synthesis and pharmacological evaluation of [18F]PBR316: a novel PET ligand targeting the translocator protein 18 kDa (TSPO) with low binding sensitivity to human single nucleotide polymorphism rs6971.

Authors:  Filomena Mattner; Andrew Katsifis; Thomas Bourdier; Christian Loc'h; Paula Berghofer; Christopher Fookes; Tzong-Tyng Hung; Timothy Jackson; David Henderson; Tien Pham; Brendan J Lee; Rachael Shepherd; Ivan Greguric; Naomi Wyatt; Thanh Le; Jackson Poon; Carl Power; Michael Fulham
Journal:  RSC Med Chem       Date:  2021-04-19

10.  Automated radiosynthesis of two 18F-labeled tracers containing 3-fluoro-2-hydroxypropyl moiety, [18F]FMISO and [18F]PM-PBB3, via [18F]epifluorohydrin.

Authors:  Takayuki Ohkubo; Yusuke Kurihara; Masanao Ogawa; Nobuki Nengaki; Masayuki Fujinaga; Wakana Mori; Katsushi Kumata; Masayuki Hanyu; Kenji Furutsuka; Hiroki Hashimoto; Kazunori Kawamura; Ming-Rong Zhang
Journal:  EJNMMI Radiopharm Chem       Date:  2021-07-10
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