Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function.
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Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptorNeurobiological Insights from mGlu Receptor Allosteric Modulation.Drugs 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 CurrentsNovel Allosteric Modulators of G Protein-coupled ReceptorsVU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo EfficacyN-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)picolinN-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats.Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity.mGlu5 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).Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu₅): from an artificial neural network virtual screen to an in vivo tool compound.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 ModulationCB1 augments mGluR5 function in medial prefrontal cortical neurons to inhibit amygdala hyperactivity in an arthritis pain model.Relationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profilesApplication of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4)Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships.Susceptibility of the adolescent brain to cannabinoids: long-term hippocampal effects and relevance to schizophrenia.Modulation of pyramidal cell output in the medial prefrontal cortex by mGluR5 interacting with CB1.A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signalingDiscovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents.Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2.Probing the metabotropic glutamate receptor 5 (mGlu₅) positive allosteric modulator (PAM) binding pocket: discovery of point mutations that engender a "molecular switch" in PAM pharmacology.Allosteric modulation and functional selectivity of G protein-coupled 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.Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptorIdentification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site.Approaches for probing allosteric interactions at 7 transmembrane spanning receptors.Metabotropic glutamate receptor 5-positive allosteric modulators for the treatment of schizophrenia (2004-2012).Activation of M1 and M4 muscarinic receptors as potential treatments for Alzheimer's disease and schizophreniaQuantitative analysis of receptor allosterism and its implication for drug discovery.Metabotropic glutamate receptor subtype 5: molecular pharmacology, allosteric modulation and stimulus biasDrug Design Strategies for GPCR Allosteric Modulators.GPR40 reduces food intake and body weight through GLP-1.Overview of Critical Parameters for the Design and Execution of a High-Throughput Screen for Allosteric Ligands.
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P2860
Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function.
description
2011 nî lūn-bûn
@nan
2011年の論文
@ja
2011年論文
@yue
2011年論文
@zh-hant
2011年論文
@zh-hk
2011年論文
@zh-mo
2011年論文
@zh-tw
2011年论文
@wuu
2011年论文
@zh
2011年论文
@zh-cn
name
Functional impact of allosteri ...... ntral nervous system function.
@ast
Functional impact of allosteri ...... ntral nervous system function.
@en
type
label
Functional impact of allosteri ...... ntral nervous system function.
@ast
Functional impact of allosteri ...... ntral nervous system function.
@en
prefLabel
Functional impact of allosteri ...... ntral nervous system function.
@ast
Functional impact of allosteri ...... ntral nervous system function.
@en
P2093
P2860
P50
P356
P1476
Functional impact of allosteri ...... entral nervous system function
@en
P2093
Alice L Rodriguez
C David Weaver
Carrie K Jones
Emily Days
Hilde Lavreysen
Hyekyung P Cho
J Scott Daniels
Jerri M Rook
Meredith J Noetzel
Paige N Vinson
P2860
P304
P356
10.1124/MOL.111.075184
P577
2011-10-21T00:00:00Z