Results 241 to 250 of about 55,850 (272)

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

Coincident modulation of adenosine receptor and metabotropic glutamate receptor 5

2021
Neurodegenerative disorders, such as Alzheimer’s disease are among the leading causes of death and disease burden. Therefore, new therapeutic targets are needed to treat both symptoms and disease progression. Glutamate and adenosine receptors are key proteins modulating brain cells’ activity.
openaire   +1 more source

Poster #S173 METABOTROPIC GLUTAMATE RECEPTOR 5 DYSREGULATION IN SCHIZOPHRENIA

Schizophrenia Research, 2014
(MBP), another myelinationand schizophrenia-related gene, is the bestcharacterized QKI mRNA ligand in mice (Larocque et al., 2002). Therefore, we tested this hypothesis using the human immature oligodendrocytic cell line, that levels of hnRNP C1 and C2 would influence the expression of these myelination-related genes. We also attempted to elucidate the
Kelly Newell, Natalie Matosin, Francesca Fernandez-Enright, Xu-Feng Huang   +3 more
openaire   +1 more source

Biased allosteric modulators of metabotropic glutamate receptor 5

2018
The metabotropic glutamate receptor 5 is involved in numerous central nervous system disorders. New ways of targeting this receptor for therapeutic benefits involve designing compounds which bind specific areas within the receptor such that unique receptor outcomes can be achieved. My thesis focused on characterising these compounds, what they are able
openaire   +1 more source

Glutamate receptor, metabotropic, type 5

AfCS-Nature Molecule Pages, 2006
Scott Duncan, Peter Koulen
openaire   +1 more source

Metabotropic Glutamate Receptor 5: A Potential Molecular Switch and Beyond

Biological Psychiatry, 2022
Zhaodi Liu, Hui Ma, Shuai Long, Yong Zhang   +3 more
openaire   +2 more sources