Results 311 to 320 of about 478,976 (349)

The Role of Metabotropic Glutamate Receptor 5 in Learning and Memory Processes

Drug News & Perspectives, 2005
Metabotropic glutamate receptor 5 (mGluR5), a subtype in the group I mGluRs, couples to phospholipase C through Gq protein. Stimulation of mGluR5 leads to the release of calcium from intracellular stores and protein kinase C activation. In addition, links to different ion channels and other signaling mechanisms have also been revealed.
Simonyi, Agnes, Schachtman, Todd, Christoffersen, Gert Rene Juul   +2 more
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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.
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The role of metabotropic glutamate receptor 5 in developmental lead neurotoxicity

Toxicology Letters, 2009
A complete explanation of the mechanisms of lead-induced developmental neurotoxicity remains unknown. The glutamate receptor is one of the most important targets of lead. More recently, metabotropic glutamate receptor 5 (mGluR5) has been shown to have a functional relationship with learning and memory.
Yu Gao, Xiaoming Shen, Xiang-yu Zou, Chonghuai Yan, Jian Xu, Ying Tian, Bo Yang, Le Zhong, Han-fang Xie   +8 more
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Design and Synthesis of Noncompetitive Metabotropic Glutamate Receptor Subtype 5 Antagonists. [PDF]

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.
Amy Hauck Newman, Richard B. Rothman, Christina M. Dersch, Barbara Nightingale, Santosh S. Kulkarni   +4 more
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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, Janice Chung, Jeffery J. Anderson, Jean Michel Vernier, Benito Munoz, Jesse Brodkin, Michael F. Gardner, Xiaoqing Yang, Xiaohui Jiang, Sara Rao   +9 more
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Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases.

Journal of Medicinal Chemistry, 2015
Negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu5) have potential for the treatment of psychiatric diseases including depression, fragile X syndrome (FXS), anxiety, obsessive-compulsive disorders, and levodopa induced ...
G. Jaeschke, S. Kolczewski, W. Spooren, E. Vieira, Nadia Bitter-Stoll, P. Boissin, E. Borroni, B. Büttelmann, S. Ceccarelli, N. Clemann, B. David, C. Funk, W. Guba, A. Harrison, T. Hartung, M. Honer, J. Huwyler, Martin Kuratli, U. Niederhauser, A. Pähler, J. Peters, Ann C. Petersen, E. Prinssen, Antonio Ricci, Daniel Rueher, Marianne Rueher, Manfred Schneider, P. Spurr, Theodor Stoll, Daniel Tännler, J. Wichmann, R. Porter, J. Wettstein, L. Lindemann   +33 more
semanticscholar   +1 more source

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
Samarjit Bhattacharyya, Rishi R. Trivedi
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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 ...
Nil Casajuana-Martin, Leonardo Pardo, Gary Tresadern, Claudia Llinas del Torrent, Laura Pérez-Benito, Laura Pérez-Benito   +5 more
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Differential effects of protein phosphatases in the recycling of metabotropic glutamate receptor 5

Neuroscience, 2015
The major excitatory neurotransmitter Glutamate acts on both ionotropic and metabotropic glutamate receptors (mGluRs) in the central nervous system. mGluR5, a member of the group I mGluR family is widely expressed throughout the brain and plays important roles in a variety of neuronal processes including various forms of synaptic plasticity.
Samarjit Bhattacharyya, Prabhat Kumar Mahato, Saurabh Pandey   +2 more
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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
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