2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist - Test2 - elhamkhani - TriplyDB

2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist

2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist

http://www.wikidata.org/entity/Q28374719

about

Synthesis, SAR and unanticipated pharmacological profiles of analogues of the mGluR5 ago-potentiator ADX-47273 Advances in the treatment of fragile X syndrome The metabotropic glutamate receptor subtype 5 antagonist fenobam is analgesic and has improved in vivo selectivity compared with the prototypical antagonist 2-methyl-6-(phenylethynyl)-pyridine Activation of metabotropic glutamate 5 (mGlu5) receptors induces spontaneous excitatory synaptic currents in layer V pyramidal cells of the rat prefrontal cortex Allosteric modulation of group III metabotropic glutamate receptor 4: a potential approach to Parkinson's disease treatment Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP Potential anxiolytic- and antidepressant-like effects of MPEP, a potent, selective and systemically active mGlu5 receptor antagonist Selective mGluR5 antagonists MPEP and SIB-1893 decrease NMDA or glutamate-mediated neuronal toxicity through actions that reflect NMDA receptor antagonism Negative Allosteric Modulators of Metabotropic Glutamate Receptors Subtype 5 in Addiction: a Therapeutic Window Fragile X syndrome and targeted treatment trials.Metabotropic glutamate receptors in the basal ganglia motor circuit Metabotropic glutamate receptors as novel targets for anxiety and stress disorders Endogenous sulphur-containing amino acids: potent agonists at presynaptic metabotropic glutamate autoreceptors in the rat central nervous system Activation of type 5 metabotropic glutamate receptors enhances NMDA responses in mice cortical wedges Structural, signalling and regulatory properties of the group I metabotropic glutamate receptors: prototypic family C G-protein-coupled receptors Novel mGluR- and CB1R-independent suppression of GABA release caused by a contaminant of the group I metabotropic glutamate receptor agonist, DHPG Group I metabotropic glutamate receptors activate a calcium-sensitive transient receptor potential-like conductance in rat hippocampus Metabotropic glutamate receptor 5 (mGluR5)-mediated phosphoinositide hydrolysis and NMDA-potentiating effects are blunted in the striatum of aged rats: a possible additional mechanism in striatal senescence Co-stimulation of mGluR5 and N-methyl-D-aspartate receptors is required for potentiation of excitatory synaptic transmission in hippocampal neurons VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy Allosteric activators of muscarinic receptors as novel approaches for treatment of CNS disorders.Blocking metabotropic glutamate receptor subtype 7 (mGlu7) via the Venus flytrap domain (VFTD) inhibits amygdala plasticity, stress, and anxiety-related behavior Substituted 1-Phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction.Fragile X: leading the way for targeted treatments in autism.Allosteric modulation of metabotropic glutamate receptors.Fragile X syndrome: mechanistic insights and therapeutic avenues regarding the role of potassium channels.(3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity.Alzheimer's disease and Down syndrome rodent models exhibit audiogenic seizures.Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology.The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors Elevated glycogen synthase kinase-3 activity in Fragile X mice: key metabolic regulator with evidence for treatment potential.Partial mGlu₅ Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects.Characterization of the metabotropic glutamate receptors mediating phospholipase C activation and calcium release in cerebellar granule cells: calcium-dependence of the phospholipase C response.Basal levels of adenosine modulate mGluR5 on rat hippocampal astrocytes.Modulation of the neuronal dopamine transporter activity by the metabotropic glutamate receptor mGluR5 in rat striatal synaptosomes through phosphorylation mediated processes.MGluR5 mediates the interaction between late-LTP, network activity, and learning Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold.β-Arrestin2 Couples Metabotropic Glutamate Receptor 5 to Neuronal Protein Synthesis and Is a Potential Target to Treat Fragile X.Repetitive self-grooming behavior in the BTBR mouse model of autism is blocked by the mGluR5 antagonist MPEP.

P2860

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P2860

2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist

http://www.wikidata.org/entity/Q28374719

description

1999 nî lūn-bûn

@nan

1999 թուականի Հոկտեմբերին հրատարակուած գիտական յօդուած

@hyw

1999 թվականի հոտեմբերին հրատարակված գիտական հոդված

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1999年の論文

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1999年論文

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1999年論文

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1999年論文

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1999年論文

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1999年論文

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1999年论文

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name

2-Methyl-6-(phenylethynyl)-pyr ...... tive mGlu5 receptor antagonist

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2-Methyl-6-(phenylethynyl)-pyr ...... tive mGlu5 receptor antagonist

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2-Methyl-6-(phenylethynyl)-pyr ...... tive mGlu5 receptor antagonist

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2-Methyl-6-(phenylethynyl)-pyr ...... tive mGlu5 receptor antagonist

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2-Methyl-6-(phenylethynyl)-pyr ...... tive mGlu5 receptor antagonist

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2-Methyl-6-(phenylethynyl)-pyr ...... tive mGlu5 receptor antagonist

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2-Methyl-6-(phenylethynyl)-pyr ...... tive mGlu5 receptor antagonist

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2-Methyl-6-(phenylethynyl)-pyr ...... tive mGlu5 receptor antagonist

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Neuropharmacology

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2-Methyl-6-(phenylethynyl)-pyr ...... tive mGlu5 receptor antagonist

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A I Sacaan

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E C Johnson

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E M Santori

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10.1016/S0028-3908(99)00082-9

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12769437

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10530811

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