Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties - Wikidata - wikimedia - TriplyDB

Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties

Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties

http://www.wikidata.org/entity/Q30498538

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An allosteric enhancer of M₄ muscarinic acetylcholine receptor function inhibits behavioral and neurochemical effects of cocaine Regulation of G protein-coupled receptors by allosteric ligands Novel Allosteric Modulators of G Protein-coupled Receptors A new mechanism of allostery in a G protein-coupled receptor dimer Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor.Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents.Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100 N-aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in preclinical models of NMDA hypofunction and cognitive enhancement.Muscarinic and nicotinic acetylcholine receptor agonists and allosteric modulators for the treatment of schizophrenia The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors Structural determinants of allosteric agonism and modulation at the M4 muscarinic acetylcholine receptor: identification of ligand-specific and global activation mechanisms.Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking.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.Crystal structures of the M1 and M4 muscarinic acetylcholine receptors Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor.Allosteric antipsychotics: m4 muscarinic potentiators as novel treatments for schizophrenia Impact of species variability and 'probe-dependence' on the detection and in vivo validation of allosteric modulation at the M4 muscarinic acetylcholine receptor.Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics A Monod-Wyman-Changeux mechanism can explain G protein-coupled receptor (GPCR) allosteric modulation Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery Polymorphism and ligand dependent changes in human glucagon-like peptide-1 receptor (GLP-1R) function: allosteric rescue of loss of function mutation.Sensing Positive versus Negative Reward Signals through Adenylyl Cyclase-Coupled GPCRs in Direct and Indirect Pathway Striatal Medium Spiny Neurons.Peptide-guided targeting of GPR55 for anti-cancer therapy.Cholinergic connectivity: it's implications for psychiatric disorders.Development of M1 mAChR allosteric and bitopic ligands: prospective therapeutics for the treatment of cognitive deficits Proposed Mode of Binding and Action of Positive Allosteric Modulators at Opioid Receptors.Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors Cholinergic contributions to the cognitive symptoms of schizophrenia and the viability of cholinergic treatments Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor.Orthosteric- and allosteric-induced ligand-directed trafficking at GPCRs.Progress in structure based drug design for G protein-coupled receptors.Muscarinic receptors: their roles in disorders of the central nervous system and potential as therapeutic targets.Emerging approaches for treatment of schizophrenia: modulation of cholinergic signaling.Approaches for probing allosteric interactions at 7 transmembrane spanning receptors.Activation of M1 and M4 muscarinic receptors as potential treatments for Alzheimer's disease and schizophrenia Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition.Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core Quantitative analysis of receptor allosterism and its implication for drug discovery.Allosteric therapies for lung cancer.

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Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties

http://www.wikidata.org/entity/Q30498538

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2009年の論文

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Molecular mechanisms of action ...... ntial antipsychotic properties

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Adrian Mogg

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Arthur Christopoulos

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Christian C Felder

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David B Shaw

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David L McKinzie

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P2860

Functional Selectivity and Classical Concepts of Quantitative Pharmacology

Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophrenia.

Evolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligand

Enhancement of D1 dopamine receptor-mediated locomotor stimulation in M(4) muscarinic acetylcholine receptor knockout mice

Qualitative and quantitative assessment of relative agonist efficacy

Selective muscarinic receptor agonist xanomeline as a novel treatment approach for schizophrenia

Effects of xanomeline, a selective muscarinic receptor agonist, on cognitive function and behavioral symptoms in Alzheimer disease.

An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission.

In vivo pharmacological characterization of the structurally novel, potent, selective mGlu2/3 receptor agonist LY404039 in animal models of psychiatric disorders.

Use of M1-M5 muscarinic receptor knockout mice as novel tools to delineate the physiological roles of the muscarinic cholinergic system.

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