Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity. - Wikidata - awgldk - TriplyDB

Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity.

Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity.

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Neurobiological Insights from mGlu Receptor Allosteric Modulation.Positive allosteric modulators of metabotropic glutamate 2 receptors in schizophrenia treatment Drugs for allosteric sites on receptors Emerging approaches for treatment of schizophrenia: modulation of glutamatergic signaling Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents N-aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in preclinical models of NMDA hypofunction and cognitive enhancement.Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolin mGlu5 positive allosteric modulation normalizes synaptic plasticity defects and motor phenotypes in a mouse model of Rett syndrome Targeting metabotropic glutamate receptors for novel treatments of schizophrenia.Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu₅).2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites.Development of allosteric modulators of GPCRs for treatment of CNS disorders Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders.Group I and group II metabotropic glutamate receptor allosteric modulators as novel potential antipsychotics.Molecular Insights into Metabotropic Glutamate Receptor Allosteric Modulation Relationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profiles Acute inhibition of neurosteroid estrogen synthesis suppresses status epilepticus in an animal model.Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors Biotransformation of a novel positive allosteric modulator of metabotropic glutamate receptor subtype 5 contributes to seizure-like adverse events in rats involving a receptor agonism-dependent mechanism.Progress toward advanced understanding of metabotropic glutamate receptors: structure, signaling and therapeutic indications Metabotropic glutamate receptor subtype 5: molecular pharmacology, allosteric modulation and stimulus bias Recent developments in the behavioural and pharmacological enhancement of extinction of drug seeking.Overview of Critical Parameters for the Design and Execution of a High-Throughput Screen for Allosteric Ligands.Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5 Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency Allosteric Modulation of GPCRs: New Insights and Potential Utility for Treatment of Schizophrenia and Other CNS Disorders.Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia.Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia.Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators.mGluR5: exploration of orthosteric and allosteric ligand binding pockets and their applications to drug discovery.Development of 1H-Pyrazolo[3,4-b]pyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators.Metabotropic Glutamatergic Receptor 5 and Stress Disorders: Knowledge Gained From Receptor Imaging Studies.Role of mGlu5 Receptors and Inhibitory Neurotransmission in M1 Dependent Muscarinic LTD in the Prefrontal Cortex: Implications in Schizophrenia.Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery.Evidence for Classical Cholinergic Toxicity Associated with Selective Activation of M1 Muscarinic Receptors.PF-06827443 Displays Robust Allosteric Agonist and Positive Allosteric Modulator Activity in High Receptor Reserve and Native Systems.Differential Pharmacology and Binding of mGlu2 Receptor Allosteric Modulators.

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P2860

Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity.

http://www.wikidata.org/entity/Q30535764

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2012 nî lūn-bûn

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2012 թուականի Նոյեմբերին հրատարակուած գիտական յօդուած

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2012 թվականի նոյեմբերին հրատարակված գիտական հոդված

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2012年の論文

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2012年論文

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2012年論文

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2012年論文

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2012年論文

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2012年論文

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J.BIOPSYCH.2012.09.012

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Biological Psychiatry

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Unique signaling profiles of p ...... fferences in in vivo activity.

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Carrie K Jones

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F Edward Dudek

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Hyekyung P Cho

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J Scott Daniels

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Jason T Manka

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Jerri M Rook

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Paige N Vinson

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Rocco D Gogliotti

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P2860

Autistic-like social behaviour in Shank2-mutant mice improved by restoring NMDA receptor function

Modification of seizure activity by electrical stimulation. II. Motor seizure

Pharmacology and functions of metabotropic glutamate receptors

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.

Cellular plasticity for group I mGluR-mediated epileptogenesis.

mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning

Interaction of N-methyl-D-aspartate and group 5 metabotropic glutamate receptors on behavioral flexibility using a novel operant set-shift paradigm.

3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity.

A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models.

N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybenzamide (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors.

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501-509

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10.1016/J.BIOPSYCH.2012.09.012

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Colleen M. Niswender

Craig W. Lindsley

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233392886

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