Literature DB >> 26743895

Metabotropic glutamate receptor 5 - a promising target in drug development and neuroimaging.

Rajapillai L I Pillai1, Dnyanesh N Tipre2.   

Abstract

This review summarizes the contributions by various teams of scientists in assessing the metabotropic glutamate receptor 5 (mGluR5) as a biomarker in neuropsychiatric disorders and diseases. Development of positive and negative allosteric modulators of mGluR5 is reviewed, as is the development of PET radioligands that have the potential to measure mGluR5 receptor density in neurological disorders and during therapeutic interventions. PET imaging provides an effective tool to assess the specificity of new drugs, select dose regimens in clinical trials, and study drug mechanisms of action. We summarize and deliver comparative analyses of mGluR5-specific PET radiotracers and their applications in understanding the pathophysiology of mGluR5-related nervous system disorders and to speed up drug development.

Entities:  

Keywords:  CNS; Drug development; Neuroimaging; Positron emission tomography; mGluR5

Mesh：

Substances：

Year:  2016        PMID： 26743895     DOI： 10.1007/s00259-015-3301-5

Source DB:  PubMed          Journal:  Eur J Nucl Med Mol Imaging        ISSN： 1619-7070            Impact factor:   9.236


  143 in total

1.  [(18)F]FPEB and [(18)F]FDEGPECO comparative study of mGlu5 quantification in rodent brain.

Authors:  Jee Hae Kang; Minkyung Lee; Young Hoon Ryu; Chul Hyoung Lyoo; Chul Hoon Kim; Kyo Chul Lee; Tae Hyun Choi; Jae Yong Choi
Journal:  Appl Radiat Isot       Date:  2015-01-28       Impact factor: 1.513

Review 2.  Use of metabotropic glutamate 5-receptor antagonists for treatment of levodopa-induced dyskinesias.

Authors:  Olivier Rascol; Susan Fox; Fabrizio Gasparini; Christopher Kenney; Thérèse Di Paolo; Baltazar Gomez-Mancilla
Journal:  Parkinsonism Relat Disord       Date:  2014-05-14       Impact factor: 4.891

3.  Radiation Dosimetry of (18)F-FPEB in Humans.

Authors:  Robert M Kessler; John Seibyl; Ronald L Cowan; David Zald; Jacob S Young; Mohammad Sib Ansari; Michael G Stabin
Journal:  J Nucl Med       Date:  2014-05-05       Impact factor: 10.057

4.  Neuroprotective activity of the mGluR5 antagonists MPEP and MTEP against acute excitotoxicity differs and does not reflect actions at mGluR5 receptors.

Authors:  Paul M Lea; Vilen A Movsesyan; Alan I Faden
Journal:  Br J Pharmacol       Date:  2005-06       Impact factor: 8.739

5.  Impaired metabotropic glutamate receptor/phospholipase C signaling pathway in the cerebral cortex in Alzheimer's disease and dementia with Lewy bodies correlates with stage of Alzheimer's-disease-related changes.

Authors:  José Luis Albasanz; Esther Dalfó; Isidro Ferrer; Mairena Martín
Journal:  Neurobiol Dis       Date:  2005-06-08       Impact factor: 5.996

6.  Syntheses and pharmacological characterization of novel thiazole derivatives as potential mGluR5 PET ligands.

Authors:  Cindy A Baumann; Linjing Mu; Nicole Wertli; Stefanie D Krämer; Michael Honer; Pius A Schubiger; Simon M Ametamey
Journal:  Bioorg Med Chem       Date:  2010-06-25       Impact factor: 3.641

7.  Species differences in mGluR5 binding sites in mammalian central nervous system determined using in vitro binding with [18F]F-PEB.

Authors:  Shil Patel; Terence G Hamill; Brett Connolly; Elaine Jagoda; Wenping Li; Raymond E Gibson
Journal:  Nucl Med Biol       Date:  2007-09-19       Impact factor: 2.408

8.  Decrease of mGluR5 receptor density goes parallel with changes in enkephalin and substance P immunoreactivity in Huntington's disease: a preliminary investigation in the postmortem human brain.

Authors:  Balázs Gulyás; Judit Sovago; Baltazar Gomez-Mancilla; Zhisheng Jia; Csaba Szigeti; Károly Gulya; Martin Schumacher; Ralph Paul Maguire; Fabrizio Gasparini; Christer Halldin
Journal:  Brain Struct Funct       Date:  2014-06-28       Impact factor: 3.270

9.  Synthesis, radiolabelling and in vitro and in vivo evaluation of a novel fluorinated ABP688 derivative for the PET imaging of metabotropic glutamate receptor subtype 5.

Authors:  Selena Milicevic Sephton; Patrick Dennler; Dominique S Leutwiler; Linjing Mu; Cindy A Wanger-Baumann; Roger Schibli; Stefanie D Krämer; Simon M Ametamey
Journal:  Am J Nucl Med Mol Imaging       Date:  2011-12-10

10.  In vivo imaging of mGluR5 changes during epileptogenesis using [11C]ABP688 PET in pilocarpine-induced epilepsy rat model.

Authors:  Hongyoon Choi; Yu Kyeong Kim; So Won Oh; Hyung-Jun Im; Do Won Hwang; Hyejin Kang; Boeun Lee; Yun-Sang Lee; Jae Min Jeong; E Edmund Kim; June-Key Chung; Dong Soo Lee
Journal:  PLoS One       Date:  2014-03-24       Impact factor: 3.240
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  10 in total

Review 1.  Metabotropic Glutamate Receptor 5 as a Target for the Treatment of Depression and Smoking: Robust Preclinical Data but Inconclusive Clinical Efficacy.

Authors:  Samuel A Barnes; Douglas J Sheffler; Svetlana Semenova; Nicholas D P Cosford; Anton Bespalov
Journal:  Biol Psychiatry       Date:  2018-03-09       Impact factor: 13.382

2.  A first-in-man PET study of [18F]PSS232, a fluorinated ABP688 derivative for imaging metabotropic glutamate receptor subtype 5.

Authors:  Geoffrey Warnock; Michael Sommerauer; Linjing Mu; Gloria Pla Gonzalez; Susanne Geistlich; Valerie Treyer; Roger Schibli; Alfred Buck; Stefanie D Krämer; Simon M Ametamey
Journal:  Eur J Nucl Med Mol Imaging       Date:  2017-11-27       Impact factor: 9.236

Review 3.  Metabotropic glutamate receptor 5 as a potential target for smoking cessation.

Authors:  Cristiano Chiamulera; Claudio Marcello Marzo; David J K Balfour
Journal:  Psychopharmacology (Berl)       Date:  2016-11-16       Impact factor: 4.530

Review 4.  Radiopharmaceuticals for PET and SPECT Imaging: A Literature Review over the Last Decade.

Authors:  George Crișan; Nastasia Sanda Moldovean-Cioroianu; Diana-Gabriela Timaru; Gabriel Andrieș; Călin Căinap; Vasile Chiș
Journal:  Int J Mol Sci       Date:  2022-04-30       Impact factor: 6.208

5.  Potential synaptic plasticity-based Shenzhiling oral liquid for a SAD Mouse Model.

Authors:  Yahan Wang; Pengwen Wang; Fang Chen; Mana Lulu; Shuaiyang Huang; Zhenhong Liu
Journal:  Brain Behav       Date:  2019-08-20       Impact factor: 2.708

6.  Analysis of the Gut Microbiota and Inflammatory Factors in mGluR5-Knockout Mice.

Authors:  Guohong Cai; Yuanyuan Zhu; Jing Chen; Suo Zhao; Liying Wang; Mengmeng Wang; Jing Huang; Shengxi Wu
Journal:  Front Psychiatry       Date:  2020-04-30       Impact factor: 4.157

7.  mGluR5 binding changes during a mismatch negativity task in a multimodal protocol with [11C]ABP688 PET/MR-EEG.

Authors:  Christoph W Lerche; Irene Neuner; Cláudia Régio Brambilla; Tanja Veselinović; Ravichandran Rajkumar; Jörg Mauler; Andreas Matusch; Andrej Ruch; Linda Orth; Shukti Ramkiran; Hasan Sbaihat; Nicolas Kaulen; Nibal Yahya Khudeish; Christine Wyss; Karsten Heekeren; Wolfram Kawohl; Elena Rota Kops; Lutz Tellmann; Jürgen Scheins; Frank Boers; Bernd Neumaier; Johannes Ermert; Markus Lang; Stefan Stüsgen; Hans Herzog; Karl-Josef Langen; N Jon Shah
Journal:  Transl Psychiatry       Date:  2022-01-10       Impact factor: 6.222

8.  Metabotropic Glutamate Receptor 5 in the Medial Prefrontal Cortex as a Molecular Determinant of Pain and Ensuing Depression.

Authors:  Geehoon Chung; Sang Jeong Kim; Sun Kwang Kim
Journal:  Front Mol Neurosci       Date:  2018-10-08       Impact factor: 5.639

9.  Revisiting the Radiosynthesis of [18F]FPEB and Preliminary PET Imaging in a Mouse Model of Alzheimer's Disease.

Authors:  Cassis Varlow; Emily Murrell; Jason P Holland; Alina Kassenbrock; Whitney Shannon; Steven H Liang; Neil Vasdev; Nickeisha A Stephenson
Journal:  Molecules       Date:  2020-02-22       Impact factor: 4.411

Review 10.  Advances in CNS PET: the state-of-the-art for new imaging targets for pathophysiology and drug development.

Authors:  Stuart P McCluskey; Christophe Plisson; Eugenii A Rabiner; Oliver Howes
Journal:  Eur J Nucl Med Mol Imaging       Date:  2019-09-21       Impact factor: 9.236
  10 in total

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