Results 231 to 240 of about 55,850 (272)

Noncanonical Metabotropic Glutamate Receptor 5 Signaling in Alzheimer's Disease

Annual Review of Pharmacology and Toxicology, 2022
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. mGluR5 supports long-term changes in synaptic strength by regulating the transcription and translation of essential synaptic proteins.
Khaled S, Abd-Elrahman, Stephen S G, Ferguson   +1 more
openaire   +2 more sources

Metabotropic glutamate receptors, 5 years on

Neuropharmacology, 2017
[no abstract]
Collingridge, Graham L., Manahan Vaughan, Denise, NICOLETTI, Ferdinando, Schoepp, Darryle D.   +3 more
openaire   +3 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 ...
Holger, Rosenbrock, Gert, Kramer, Scott, Hobson, Eliza, Koros, Marc, Grundl, Matthias, Grauert, Klaus G, Reymann, Ulrich H, Schröder   +7 more
openaire   +2 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   +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 ...
Lindstrom, E., Brusberg, M., Hughes, P., Martin, C., Brierley, S., Phillis, B., Martinsson, R., Abrahamsson, C., Larsson, H., Martinez, V., Blackshaw, L.   +10 more
openaire   +3 more sources

Dipyridyl amines: Potent metabotropic glutamate subtype 5 receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2005
Modulation of the metabotropic glutamate subtype 5 (mGlu5) receptor may be useful in the treatment of a variety of central nervous system disorders. Herein, we report on the discovery, synthesis, and biological evaluation of dipyridyl amines as small molecule mGlu5 antagonists.
Theodore M, Kamenecka, Céline, Bonnefous, Steven, Govek, Jean-Michel, Vernier, John, Hutchinson, Janice, Chung, Grace, Reyes-Manalo, Jeffery J, Anderson   +7 more
openaire   +2 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   +3 more sources

Metabotropic glutamate receptor type 5 in levodopa-induced motor complications

Neurobiology of Aging, 2011
Metabotropic glutamate receptors type 5 (mGluR5) are implicated in regulation of synaptic plasticity and learning, and were the focus of our investigation in human Parkinson's disease (PD) patients with dyskinesias and wearing-off, and in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) monkeys with dyskinesias. Using the selective mGluR5 ligand [(3)
Bazoumana, Ouattara, Laurent, Grégoire, Marc, Morissette, Fabrizio, Gasparini, Ivo, Vranesic, Graeme, Bilbe, Donald R, Johns, Alex, Rajput, Oleh, Hornykiewicz, Ali H, Rajput, Baltazar, Gomez-Mancilla, Thérèse, Di Paolo   +11 more
openaire   +2 more sources

Mechanisms Underlying Allosteric Molecular Switches of Metabotropic Glutamate Receptor 5

Journal of Chemical Information and Modeling, 2019
The metabotropic glutamate 5 (mGlu5) receptor is a class C G protein-coupled receptor (GPCR) that is implicated in several CNS disorders making it a popular drug discovery target. Years of research have revealed allosteric mGlu5 ligands showing an unexpected complete switch in functional activity despite only small changes in their chemical structure ...
Claudia Llinas del Torrent, Nil Casajuana-Martin, Leonardo Pardo, Gary Tresadern, Laura Pérez-Benito   +4 more
openaire   +2 more sources

Biased agonism and allosteric modulation of metabotropic glutamate receptor 5

Clinical Science, 2018
Metabotropic glutamate receptors belong to class C G-protein-coupled receptors and consist of eight subtypes that are ubiquitously expressed throughout the central nervous system. In recent years, the metabotropic glutamate receptor subtype 5 (mGlu5) has emerged as a promising target for a broad range of psychiatric and neurological disorders.
Phuc N.H. Trinh, Lauren T. May, Katie Leach, Karen J. Gregory   +3 more
openaire   +2 more sources