Results 201 to 210 of about 54,795 (218)

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

Discovery of novel modulators of metabotropic glutamate receptor subtype-5

Bioorganic & Medicinal Chemistry, 2004
A series of potent and selective mGluR5 antagonists were synthesized and evaluated in vitro and in vivo. It was found that a pyridyl functionality is a potential replacement for acetonitrile in the lead structure, with 2-pyridyl being most favored.
Bowei, Wang, Jean Michel, Vernier, Sara, Rao, Janice, Chung, Jeffery J, Anderson, Jesse D, Brodkin, Xiaohui, Jiang, Michael F, Gardner, Xiaoqing, Yang, Benito, Munoz   +9 more
openaire   +2 more sources

Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2005
The mGlu5 receptor has been implicated in a number of CNS disorders. Herein, we report on the discovery, synthesis, and biological evaluation of dipyridyl amides as small molecules mGluR5 antagonists.
Céline, Bonnefous, Jean-Michel, Vernier, John H, Hutchinson, Janice, Chung, Grace, Reyes-Manalo, Theodore, Kamenecka   +5 more
openaire   +2 more sources

Constitutive internalization and recycling of metabotropic glutamate receptor 5 (mGluR5)

Biochemical and Biophysical Research Communications, 2012
Ligand-dependent and ligand-independent endocytic trafficking of G-protein coupled receptors (GPCRs) is critical for accurate receptor-mediated signaling and its regulation. Metabotropic glutamate receptor 5 (mGluR5) is a GPCR that plays a crucial role in circuit formation in the brain and also in various forms of synaptic plasticity including learning
Rishi Raj, Trivedi, Samarjit, Bhattacharyya   +1 more
openaire   +2 more sources

Design and Synthesis of Noncompetitive Metabotropic Glutamate Receptor Subtype 5 Antagonists.

ChemInform, 2006
AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Santosh S, Kulkarni, Barbara, Nightingale, Christina M, Dersch, Richard B, Rothman, Amy Hauck, Newman   +4 more
openaire   +2 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 ...
J V, Berger, A O, Dumont, M C, Focant, M, Vergouts, A, Sternotte, A-G, Calas, S, Goursaud, E, Hermans   +7 more
openaire   +2 more sources