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Synthesis toward Bivalent Ligands for the Dopamine D2 and Metabotropic Glutamate 5 Receptors.
Journal of Medicinal Chemistry, 2018In this study, we designed and synthesized heterobivalent ligands targeting heteromers consisting of the metabotropic glutamate 5 receptor (mGluR5) and the dopamine D2 receptor (D2R). Bivalent ligand 22a with a linker consisting of 20 atoms showed 4-fold
Mingcheng Qian +8 more
semanticscholar +1 more source
Metabotropic glutamate receptor 5 in the pathology and treatment of schizophrenia
Neuroscience & Biobehavioral Reviews, 2013Metabotropic 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
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Molecular Pharmacology, 2003
Metabotropic glutamate (mGlu) 5 is a G-protein-coupled metabotropic glutamate receptor that plays an important role as a modulator of synaptic plasticity, ion channel activity, and excitotoxicity.
P. Malherbe +7 more
semanticscholar +1 more source
Metabotropic glutamate (mGlu) 5 is a G-protein-coupled metabotropic glutamate receptor that plays an important role as a modulator of synaptic plasticity, ion channel activity, and excitotoxicity.
P. Malherbe +7 more
semanticscholar +1 more source
Selective blockade of metabotropic glutamate receptor subtype 5 is neuroprotective
Neuropharmacology, 2000We 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 +9 more
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Journal of Medicinal Chemistry, 2006
CDPPB [3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide] was recently described as the first centrally active, positive allosteric modulator of rat and human metabotropic glutamate receptor (mGluR) mGluR5 subtype. We explored the structural requirements
T. de Paulis +8 more
semanticscholar +1 more source
CDPPB [3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide] was recently described as the first centrally active, positive allosteric modulator of rat and human metabotropic glutamate receptor (mGluR) mGluR5 subtype. We explored the structural requirements
T. de Paulis +8 more
semanticscholar +1 more source
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 +7 more
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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 +7 more
openaire +3 more sources
Recent Patents on CNS Drug Discovery, 2010
The glutamate hypothesis of schizophrenia suggests that hypofunction of N-methyl-D-aspartate (NMDA) receptors may be critical for schizophrenic symptoms; therefore, pharmacological approaches that enhance NMDA function may be beneficial for the treatment
K. Kanuma, T. Aoki, Youichi Shimazaki
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The glutamate hypothesis of schizophrenia suggests that hypofunction of N-methyl-D-aspartate (NMDA) receptors may be critical for schizophrenic symptoms; therefore, pharmacological approaches that enhance NMDA function may be beneficial for the treatment
K. Kanuma, T. Aoki, Youichi Shimazaki
semanticscholar +1 more source
Non-competitive inhibitors of metabotropic glutamate receptor 5 (mGluR5)
Bioorganic & Medicinal Chemistry Letters, 2005Based 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 +7 more
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Biased agonism and allosteric modulation of metabotropic glutamate receptor 5 [PDF]
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 +3 more
openaire +2 more sources
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 +13 more
semanticscholar +1 more source
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 +13 more
semanticscholar +1 more source