Literature DB >> 31879207

Synthesis and evaluation of 6-(11C-methyl(4-(pyridin-2-yl)thiazol-2-yl)amino)benzo[d]thiazol-2(3H)-one for imaging γ-8 dependent transmembrane AMPA receptor regulatory protein by PET.

Qingzhen Yu1, Katsushi Kumata2, Hua Li1, Yiding Zhang2, Zhen Chen1, Xiaofei Zhang1, Tuo Shao1, Akiko Hatori2, Tomoteru Yamasaki2, Lin Xie2, Kuan Hu2, Gangqiang Wang3, Lee Josephson1, Shaofa Sun4, Ming-Rong Zhang5, Steven H Liang6.   

Abstract

Transmembrane AMPA receptor regulatory proteins (TARPs) are a recently discovered family of proteins that modulate AMPA receptors activity. Based on a potent and selective TARP subtype γ-8 antagonist, 6-(methyl(4-(pyridin-2-yl)thiazol-2-yl)amino)benzo[d]thiazol-2(3H)-one (compound 9), we perform the radiosynthesis of its 11C-isotopologue 1 and conduct preliminary PET evaluation to test the feasibility of imaging TARP γ-8 dependent receptors in vivo.
Copyright © 2019 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  AMPA; Carbon-11; Positron emission tomography; TARP; Transmembrane AMPA receptor regulatory proteins

Year:  2019        PMID： 31879207      PMCID： PMC7045276          DOI： 10.1016/j.bmcl.2019.126879

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


  34 in total

1.  An emerging role for TARPs in neuropsychiatric disorders.

Authors:  Martin B Gill; David S Bredt
Journal:  Neuropsychopharmacology       Date:  2011-01       Impact factor: 7.853

2.  Closing in on the AMPA receptor: synthesis and evaluation of 2-acetyl-1-(4'-chlorophenyl)-6-methoxy-7-[11C]methoxy-1,2,3,4-tetrahydroisoquinoline as a potential PET tracer.

Authors:  Erik Arstad; Rosaria Gitto; Alba Chimirri; Roberta Caruso; Andrew Constanti; David Turton; Sue P Hume; Rabia Ahmad; Lyn S Pilowsky; Sajinder K Luthra
Journal:  Bioorg Med Chem       Date:  2006-04-18       Impact factor: 3.641

3.  Shiga toxin-mediated retrograde delivery of a topoisomerase I inhibitor prodrug.

Authors:  Abdessamad El Alaoui; Frédéric Schmidt; Mohamed Amessou; Marianne Sarr; Didier Decaudin; Jean-Claude Florent; Ludger Johannes
Journal:  Angew Chem Int Ed Engl       Date:  2007       Impact factor: 15.336

4.  Virtually instantaneous, room-temperature [(11)C]-cyanation using biaryl phosphine Pd(0) complexes.

Authors:  Hong Geun Lee; Phillip J Milner; Michael S Placzek; Stephen L Buchwald; Jacob M Hooker
Journal:  J Am Chem Soc       Date:  2015-01-09       Impact factor: 15.419

5.  Spatial diversity in gene expression for VDCCgamma subunit family in developing and adult mouse brains.

Authors:  Masahiro Fukaya; Maya Yamazaki; Kenji Sakimura; Masahiko Watanabe
Journal:  Neurosci Res       Date:  2005-09-19       Impact factor: 3.304

Review 6.  AMPA receptors as drug targets in neurological disease--advantages, caveats, and future outlook.

Authors:  Philip K-Y Chang; David Verbich; R Anne McKinney
Journal:  Eur J Neurosci       Date:  2012-06       Impact factor: 3.386

7.  "In-loop" [11 C]CO2 fixation: Prototype and proof of concept.

Authors:  Kenneth Dahl; Thomas L Collier; Ran Cheng; Xiaofei Zhang; Oleg Sadovski; Steven H Liang; Neil Vasdev
Journal:  J Labelled Comp Radiopharm       Date:  2017-07-25       Impact factor: 1.921

8.  Synthesis, pharmacology and preclinical evaluation of 11C-labeled 1,3-dihydro-2H-benzo[d]imidazole-2-ones for imaging γ8-dependent transmembrane AMPA receptor regulatory protein.

Authors:  Zhen Chen; Wakana Mori; Xiaofei Zhang; Tomoteru Yamasaki; Patrick J Dunn; Genwei Zhang; Hualong Fu; Tuo Shao; Yiding Zhang; Akiko Hatori; Longle Ma; Masayuki Fujinaga; Lin Xie; Xiaoyun Deng; Hua Li; Qingzhen Yu; Jian Rong; Lee Josephson; Jun-An Ma; Yihan Shao; Susumu Tomita; Ming-Rong Zhang; Steven H Liang
Journal:  Eur J Med Chem       Date:  2018-08-09       Impact factor: 6.514

Review 9.  Determination of lipophilicity and its use as a predictor of blood-brain barrier penetration of molecular imaging agents.

Authors:  Rikki N Waterhouse
Journal:  Mol Imaging Biol       Date:  2003 Nov-Dec       Impact factor: 3.488

10.  Radiosynthesis and preliminary PET evaluation of (18)F-labeled 2-(1-(3-fluorophenyl)-2-oxo-5-(pyrimidin-2-yl)-1,2-dihydropyridin-3-yl)benzonitrile for imaging AMPA receptors.

Authors:  Gengyang Yuan; Graham B Jones; Neil Vasdev; Steven H Liang
Journal:  Bioorg Med Chem Lett       Date:  2016-08-09       Impact factor: 2.823
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