Literature DB >> 21115250

The first synthesis of [(11)C]SB-216763, a new potential PET agent for imaging of glycogen synthase kinase-3 (GSK-3).

Min Wang1, Mingzhang Gao, Kathy D Miller, George W Sledge, Gary D Hutchins, Qi-Huang Zheng.   

Abstract

SB-216763 is a novel, potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor with an IC(50) value of 34 nM. [(11)C]SB-216763 (3-(2,4-dichlorophenyl)-4-(1-[(11)C]methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione), a new potential PET agent for imaging of GSK-3, was first designed and synthesized in 20-30% decay corrected radiochemical yield and 370-555 GBq/μmol specific activity at end of bombardment (EOB). The synthetic strategy was to prepare a carbon-11-labeled maleic anhydride intermediate followed by the conversion to maleimide.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 21115250     DOI： 10.1016/j.bmcl.2010.11.026

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


  9 in total

1.  Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging.

Authors:  Steven H Liang; Jinshan Michael Chen; Marc D Normandin; Jeanne S Chang; George C Chang; Christine K Taylor; Patrick Trapa; Mark S Plummer; Kimberly S Para; Edward L Conn; Lori Lopresti-Morrow; Lorraine F Lanyon; James M Cook; Karl E G Richter; Charlie E Nolan; Joel B Schachter; Fouad Janat; Ye Che; Veerabahu Shanmugasundaram; Bruce A Lefker; Bradley E Enerson; Elijahu Livni; Lu Wang; Nicolas J Guehl; Debasis Patnaik; Florence F Wagner; Roy Perlis; Edward B Holson; Stephen J Haggarty; Georges El Fakhri; Ravi G Kurumbail; Neil Vasdev
Journal:  Angew Chem Int Ed Engl       Date:  2016-06-29       Impact factor: 15.336

2.  Synthesis and Initial in Vivo Studies with [(11)C]SB-216763: The First Radiolabeled Brain Penetrative Inhibitor of GSK-3.

Authors:  Lei Li; Xia Shao; Erin L Cole; Stephan A Ohnmacht; Valentina Ferrari; Young T Hong; David J Williamson; Tim D Fryer; Carole A Quesada; Phillip Sherman; Patrick J Riss; Peter J H Scott; Franklin I Aigbirhio
Journal:  ACS Med Chem Lett       Date:  2015-03-10       Impact factor: 4.345

3.  Synthesis and evaluation of [(11)C]PyrATP-1, a novel radiotracer for PET imaging of glycogen synthase kinase-3β (GSK-3β).

Authors:  Erin L Cole; Xia Shao; Phillip Sherman; Carole Quesada; Maria V Fawaz; Timothy J Desmond; Peter J H Scott
Journal:  Nucl Med Biol       Date:  2014-04-02       Impact factor: 2.408

4.  Radiosynthesis and in Vivo Evaluation of [11C]A1070722, a High Affinity GSK-3 PET Tracer in Primate Brain.

Authors:  Jaya Prabhakaran; Francesca Zanderigo; Kiran Kumar Solingapuram Sai; Harry Rubin-Falcone; Matthew J Jorgensen; Jay R Kaplan; Akiva Mintz; J John Mann; J S Dileep Kumar
Journal:  ACS Chem Neurosci       Date:  2017-05-17       Impact factor: 4.418

5.  Development of [18F]Maleimide-Based Glycogen Synthase Kinase-3β Ligands for Positron Emission Tomography Imaging.

Authors:  Kongzhen Hu; Debasis Patnaik; Thomas Lee Collier; Katarzyna N Lee; Han Gao; Matthew R Swoyer; Benjamin H Rotstein; Hema S Krishnan; Steven H Liang; Jin Wang; Zhiqiang Yan; Jacob M Hooker; Neil Vasdev; Stephen J Haggarty; Ming-Yu Ngai
Journal:  ACS Med Chem Lett       Date:  2017-02-02       Impact factor: 4.345

6.  The pivotal role of glycogen synthase kinase 3 (GSK-3) in vomiting evoked by specific emetogens in the least shrew (Cryptotis parva).

Authors:  W Zhong; N A Darmani
Journal:  Neurochem Int       Date:  2019-11-15       Impact factor: 3.921

Review 7.  Glycogen Synthase Kinase-3 Inhibitors: Preclinical and Clinical Focus on CNS-A Decade Onward.

Authors:  Sara Melisa Arciniegas Ruiz; Hagit Eldar-Finkelman
Journal:  Front Mol Neurosci       Date:  2022-01-21       Impact factor: 5.639

Review 8.  Glycogen Synthase Kinase-3 (GSK-3)-Targeted Therapy and Imaging.

Authors:  Mukesh K Pandey; Timothy R DeGrado
Journal:  Theranostics       Date:  2016-02-17       Impact factor: 11.556

Review 9.  Emerging PET Radiotracers and Targets for Imaging of Neuroinflammation in Neurodegenerative Diseases: Outlook Beyond TSPO.

Authors:  Vidya Narayanaswami; Kenneth Dahl; Vadim Bernard-Gauthier; Lee Josephson; Paul Cumming; Neil Vasdev
Journal:  Mol Imaging       Date:  2018 Jan-Dec       Impact factor: 4.488
  9 in total

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