Literature DB >> 20583985

Radioligands for the PET imaging of metabotropic glutamate receptor subtype 5 (mGluR5).

Linjing Mu1, P August Schubiger, Simon M Ametamey.   

Abstract

Metabotropic glutamate receptors (mGluRs) are G-protein coupled receptors (GPCR), which activate intracellular secondary messenger systems when bound by the physiological ligand glutamate. Modulation of mGluR5s has potential for the treatment of variety of psychiatric and neurological diseases such as depression, anxiety, schizophrenia and Parkinson's disease. Positron emission tomography (PET) might offer the possibility to visualize the mGluR5 and present an interesting tool for studying this receptor-subtype under physiologic and pathologic conditions. In this review paper, emphasis is given to the radiosynthesis, in vitro and in vivo characterization of recently published mGluR5 PET tracers.

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Year:  2010        PMID： 20583985     DOI： 10.2174/156802610793176783

Source DB:  PubMed          Journal:  Curr Top Med Chem        ISSN： 1568-0266            Impact factor:   3.295


  12 in total

1.  PET imaging of metabotropic glutamate receptor subtype 5 (mGluR5).

Authors:  Dan Li; Hong Shan; Peter Conti; Zibo Li
Journal:  Am J Nucl Med Mol Imaging       Date:  2011-12-15

2.  Relationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profiles.

Authors:  Jerri M Rook; Mohammed N Tantawy; Mohammad S Ansari; Andrew S Felts; Shaun R Stauffer; Kyle A Emmitte; Robert M Kessler; Colleen M Niswender; J Scott Daniels; Carrie K Jones; Craig W Lindsley; P Jeffrey Conn
Journal:  Neuropsychopharmacology       Date:  2014-09-22       Impact factor: 7.853

Review 3.  Considerations in the Development of Reversibly Binding PET Radioligands for Brain Imaging.

Authors:  Victor W Pike
Journal:  Curr Med Chem       Date:  2016       Impact factor: 4.530

4.  Drug Design Strategies for GPCR Allosteric Modulators.

Authors:  P Jeffrey Conn; Scott D Kuduk; Darío Doller
Journal:  Annu Rep Med Chem       Date:  2012       Impact factor: 1.059

Review 5.  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

6.  [carbonyl-11C]4-Fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([11C]FIMX) is an effective radioligand for PET imaging of metabotropic glutamate receptor 1 (mGluR1) in monkey brain.

Authors:  Jinsoo Hong; Shuiyu Lu; Rong Xu; Jeih-San Liow; Alicia E Woock; Kimberly J Jenko; Robert L Gladding; Sami S Zoghbi; Robert B Innis; Victor W Pike
Journal:  Nucl Med Biol       Date:  2015-07-23       Impact factor: 2.408

7.  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

Review 8.  Negative Allosteric Modulators of Metabotropic Glutamate Receptors Subtype 5 in Addiction: a Therapeutic Window.

Authors:  Yoan Mihov; Gregor Hasler
Journal:  Int J Neuropsychopharmacol       Date:  2016-07-05       Impact factor: 5.176

9.  Improved Syntheses of the Mglu₅ Antagonists MMPEP and MTEP Using Sonogashira Cross-Coupling.

Authors:  Boshuai Mu; Linjing Mu; Roger Schibli; Simon M Ametamey; Selena Milicevic Sephton
Journal:  Pharmaceuticals (Basel)       Date:  2018-02-20

Review 10.  Precision Medicine in Multiple Sclerosis: Future of PET Imaging of Inflammation and Reactive Astrocytes.

Authors:  Pekka Poutiainen; Merja Jaronen; Francisco J Quintana; Anna-Liisa Brownell
Journal:  Front Mol Neurosci       Date:  2016-09-15       Impact factor: 5.639
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