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Noncanonical Metabotropic Glutamate Receptor 5 Signaling in Alzheimer's Disease. [PDF]

Annual Review of Pharmacology and Toxicology, 2021
Metabotropic glutamate receptor 5 (mGluR5) is ubiquitously expressed in brain regions responsible for memory and learning. It plays a key role in modulating rapid changes in synaptic transmission and plasticity.
Khaled S. Abd-Elrahman, Stephen S. G. Ferguson   +1 more
semanticscholar   +3 more sources

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Metabotropic Glutamate Receptor 5 in Natural Killer Cells Attenuates Liver Fibrosis by Exerting Cytotoxicity to Activated Stellate Cells

Hepatology, 2021
The important roles of glutamate and metabotropic glutamate receptor 5 (mGluR5) in HSCs have recently been reported in various liver diseases; however, the mechanism linking the glutamine/glutamate metabolism and mGluR5 in liver fibrosis remains unclear.
Won-Mook Choi, Tom Ryu, Jun‐Hee Lee, Young-Ri Shim, Myung-Ho Kim, Hee-Hoon Kim, Y. Kim, Keungmo Yang, Kyurae Kim, Sung-E Choi, Won Kim, Seok-Hwan Kim, H. Eun, W. Jeong   +13 more
semanticscholar   +1 more source

Metabotropic glutamate receptors, 5 years on

Neuropharmacology, 2017
[no abstract]
Collingridge, Graham L., Manahan Vaughan, Denise, NICOLETTI, Ferdinando, Schoepp, Darryle D.   +3 more
openaire   +4 more sources

The metabotropic glutamate receptor 5 as a biomarker for psychiatric disorders

2023
The role of glutamate system in the etiology and pathophysiology of psychiatric disorders has gained considerable attention in the past two decades, including dysregulation of the metabotropic glutamatergic receptor subtype 5 (mGlu5). Thus, mGlu5 may represent a promising therapeutic target for psychiatric conditions, particularly stress-related ...
Ruth H, Asch, Ansel T, Hillmer, Stephen R, Baldassarri, Irina, Esterlis   +3 more
openaire   +2 more sources

Functional interaction of metabotropic glutamate receptor 5 and NMDA-receptor by a metabotropic glutamate receptor 5 positive allosteric modulator

European Journal of Pharmacology, 2010
The NMDA (N-methyl-D-aspartate)-receptor is fundamentally involved in cognitive functions. Recent studies demonstrated a functional interaction between the metabotropic glutamate receptor 5 (mGlu(5) receptor) and the NMDA-receptor in neurons. In rat hippocampal slices, it was shown that activation of mGlu(5) receptor by a positive modulator in the ...
Marc Grundl, Eliza Koros, Gert Kramer, Ulrich H. Schröder, Klaus G. Reymann, Scott Hobson, Matthias Grauert, Holger Rosenbrock   +7 more
openaire   +3 more sources

Metabotropic glutamate receptor 5 in the pathology and treatment of schizophrenia

Neuroscience & Biobehavioral Reviews, 2013
Metabotropic glutamate receptor 5 (mGluR5) potentiates the NMDA receptor (NMDAR) in brain regions implicated in schizophrenia, making it a viable therapeutic target for the treatment of this disorder. mGluR5 positive allosteric modulators may represent a valuable novel strategy for schizophrenia treatment, given the favourable profile of effects in ...
Matosin, Natalie, Newell, Kelly A
openaire   +3 more sources

Involvement of metabotropic glutamate 5 receptor in visceral pain

Pain, 2008
Metabotropic glutamate 5 receptor (mGluR5) antagonists are effective in animal models of inflammatory and neuropathic pain. The involvement of mGluR5 in visceral pain pathways from the gastrointestinal tract is as yet unknown. We evaluated effects of mGluR5 antagonists on the colorectal distension (CRD)-evoked visceromotor (VMR) and cardiovascular ...
Rakel Martinsson, Vicente Martinez, Christina Abrahamsson, Stuart M. Brierley, Stuart M. Brierley, Christopher M. Martin, Patrick A. Hughes, Patrick A. Hughes, Håkan Larsson, Benjamin D. Phillis, Benjamin D. Phillis, Mikael Brusberg, Erik Lindström, L. Ashley Blackshaw, L. Ashley Blackshaw   +14 more
openaire   +4 more sources

Selective blockade of metabotropic glutamate receptor subtype 5 is neuroprotective

Neuropharmacology, 2000
We have used potent and selective non-competitive antagonists of metabotropic glutamate receptor subtype 5 (mGlu5) -- 2-methyl-6-phenylethynylpyridine (MPEP), [6-methyl-2-(phenylazo)-3-pyridinol] (SIB-1757) and [(E)-2-methyl-6-(2-phenylethenyl)pyridine] (SIB-1893) - to examine whether endogenous activation of this particular metabotropic glutamate ...
BRUNO, Valeria Maria Gloria, KSIAZEK I, BATTAGLIA, Giuseppe, LUKIC S, LEONHARD T, SAUER D, GASPARINI F, KUHN R, NICOLETTI, Ferdinando, FLOR PJ   +9 more
openaire   +4 more sources

Opposite regulation of metabotropic glutamate receptor 3 and metabotropic glutamate receptor 5 by inflammatory stimuli in cultured microglia and astrocytes

Neuroscience, 2012
Metabotropic glutamate receptors (mGluRs) were previously shown to modulate several essential functions in glial cells, including cell proliferation, glutamate uptake, neurotrophic support, and inflammatory responses. As these receptors are regularly proposed as promising targets for the treatment of a wide range of neurological disorders, we herein ...
Julie V Berger, Marylène C. Focant, Emmanuel Hermans, Stéphanie Goursaud, Maxime Vergouts, André-Guilhem Calas, Amélie Dumont, Anthony Sternotte   +7 more
openaire   +3 more sources

Non-competitive inhibitors of metabotropic glutamate receptor 5 (mGluR5)

Bioorganic & Medicinal Chemistry Letters, 2005
Based on a pharmacophore alignment on known non-competitive mGluR5 inhibitors applying 4SCan technology, a new lead series was identified and further structurally investigated. K(i)'s as low as around 100 nM were achieved.
Tasler S, Kraus M, Pegoraro S, Aschenbrenner A, Poggesi E, Testa R, MOTTA, Gaetano, Leonardi A.   +7 more
openaire   +4 more sources