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 treatmentDrugs for allosteric sites on receptorsEmerging approaches for treatment of schizophrenia: modulation of glutamatergic signalingBiased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR CurrentsN-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)picolinmGlu5 positive allosteric modulation normalizes synaptic plasticity defects and motor phenotypes in a mouse model of Rett syndromeTargeting 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 disordersOpportunities 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 ModulationRelationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profilesAcute 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 ReceptorsBiotransformation 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 indicationsMetabotropic glutamate receptor subtype 5: molecular pharmacology, allosteric modulation and stimulus biasRecent 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 mGluR5Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiencyAllosteric 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 TypeDiscovery 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 penetrationAcyl 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.
P2860
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P2860
Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity.
description
2012 nî lūn-bûn
@nan
2012 թուականի Նոյեմբերին հրատարակուած գիտական յօդուած
@hyw
2012 թվականի նոյեմբերին հրատարակված գիտական հոդված
@hy
2012年の論文
@ja
2012年論文
@yue
2012年論文
@zh-hant
2012年論文
@zh-hk
2012年論文
@zh-mo
2012年論文
@zh-tw
2012年论文
@wuu
name
Unique signaling profiles of p ...... fferences in in vivo activity.
@ast
Unique signaling profiles of p ...... fferences in in vivo activity.
@en
type
label
Unique signaling profiles of p ...... fferences in in vivo activity.
@ast
Unique signaling profiles of p ...... fferences in in vivo activity.
@en
prefLabel
Unique signaling profiles of p ...... fferences in in vivo activity.
@ast
Unique signaling profiles of p ...... fferences in in vivo activity.
@en
P2093
P2860
P50
P1476
Unique signaling profiles of p ...... fferences in in vivo activity.
@en
P2093
Carrie K Jones
F Edward Dudek
Hyekyung P Cho
J Scott Daniels
Jason T Manka
Jerri M Rook
Karen J Gregory
Meredith J Noetzel
Paige N Vinson
Rocco D Gogliotti
P2860
P304
P356
10.1016/J.BIOPSYCH.2012.09.012
P407
P577
2012-11-07T00:00:00Z