Literature DB >> 20138515

Synthesis and in vitro evaluation of (18)F-labelled S-fluoroalkyl diarylguanidines: Novel high-affinity NMDA receptor antagonists for imaging with PET.

Edward G Robins1, Yongjun Zhao, Imtiaz Khan, Anthony Wilson, Sajinder K Luthra, Erik Rstad.   

Abstract

Two S-[(18)F]fluoroalkylated diarylguanidines were synthesized and evaluated in vitro as potential tracers for imaging of N-methyl-d-aspartate receptors (NMDARs) with positron emission tomography (PET). [(18)F]1 and [(18)F]10 were synthesized by [(18)F]fluoroethylation and [(18)F]fluoromethylation of the thiol precursor 6, respectively. [(18)F]1 is a promising candidate NMDAR PET tracer, with low nanomolar affinity for the NMDA PCP-site, high selectivity and moderate lipophilicity. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20138515     DOI： 10.1016/j.bmcl.2010.01.052

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


  11 in total

Review 1.  Positron Emission Tomography (PET) Ligand Development for Ionotropic Glutamate Receptors: Challenges and Opportunities for Radiotracer Targeting N-Methyl-d-aspartate (NMDA), α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA), and Kainate Receptors.

Authors:  Hualong Fu; Zhen Chen; Lee Josephson; Zijing Li; Steven H Liang
Journal:  J Med Chem       Date:  2018-08-27       Impact factor: 7.446

2.  New N-aryl-N'-(3-(substituted)phenyl)-N'-methylguanidines as leads to potential PET radioligands for imaging the open NMDA receptor.

Authors:  Gregory R Naumiec; Lisheng Cai; Victor W Pike
Journal:  Bioorg Med Chem Lett       Date:  2014-11-29       Impact factor: 2.823

Review 3.  Selected PET Radioligands for Ion Channel Linked Neuroreceptor Imaging: Focus on GABA, NMDA and nACh Receptors.

Authors:  Alina Kassenbrock; Neil Vasdev; Steven H Liang
Journal:  Curr Top Med Chem       Date:  2016       Impact factor: 3.295

4.  NMDA receptor ion channel activation detected in vivo with [18F]GE-179 PET after electrical stimulation of rat hippocampus.

Authors:  Ali K Vibholm; Anne M Landau; Arne Møller; Jan Jacobsen; Kim Vang; Ole L Munk; Dariusz Orlowski; Jens Ch Sørensen; David J Brooks
Journal:  J Cereb Blood Flow Metab       Date:  2020-09-22       Impact factor: 6.200

5.  In Vivo [18F]GE-179 Brain Signal Does Not Show NMDA-Specific Modulation with Drug Challenges in Rodents and Nonhuman Primates.

Authors:  Matthias Schoenberger; Frederick A Schroeder; Michael S Placzek; Randall L Carter; Bruce R Rosen; Jacob M Hooker; Christin Y Sander
Journal:  ACS Chem Neurosci       Date:  2017-11-14       Impact factor: 4.418

6.  N'-3-(Trifluoromethyl)phenyl Derivatives of N-Aryl-N'-methylguanidines as Prospective PET Radioligands for the Open Channel of the N-Methyl-d-aspartate (NMDA) Receptor: Synthesis and Structure-Affinity Relationships.

Authors:  Gregory R Naumiec; Kimberley J Jenko; Sami S Zoghbi; Robert B Innis; Lisheng Cai; Victor W Pike
Journal:  J Med Chem       Date:  2015-12-04       Impact factor: 7.446

Review 7.  Development of PET and SPECT probes for glutamate receptors.

Authors:  Takeshi Fuchigami; Morio Nakayama; Sakura Yoshida
Journal:  ScientificWorldJournal       Date:  2015-03-22

8.  Binding characterization of N-(2-chloro-5-thiomethylphenyl)-N'-(3-[3 H]3 methoxy phenyl)-N'-methylguanidine ([3 H]GMOM), a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist.

Authors:  Athanasios Metaxas; Bart N M van Berckel; Pieter J Klein; Joost Verbeek; Emily C Nash; Esther J M Kooijman; Véronique A Renjaän; Sandeep S V Golla; Ronald Boellaard; Johannes A M Christiaans; Albert D Windhorst; Josée E Leysen
Journal:  Pharmacol Res Perspect       Date:  2019-02

9.  Quantification of the novel N-methyl-d-aspartate receptor ligand [11C]GMOM in man.

Authors:  Thalia F van der Doef; Sandeep S V Golla; Pieter J Klein; Gisela M Oropeza-Seguias; Robert C Schuit; Athanasios Metaxas; Ellen Jobse; Lothar A Schwarte; Albert D Windhorst; Adriaan A Lammertsma; Bart N M van Berckel; Ronald Boellaard
Journal:  J Cereb Blood Flow Metab       Date:  2015-10-05       Impact factor: 6.200

10.  RGS4 deficit in prefrontal cortex contributes to the behaviors related to schizophrenia via system xc--mediated glutamatergic dysfunction in mice.

Authors:  Min-Wei Huang; Yu-Jung Lin; Chi-Wei Chang; Fu-Ju Lei; En-Peng Ho; Ren-Shyan Liu; Woei-Cherng Shyu; Chia-Hung Hsieh
Journal:  Theranostics       Date:  2018-09-09       Impact factor: 11.556
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