Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100 - Test2 - elhamkhani - TriplyDB

Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100

Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100

http://www.wikidata.org/entity/Q30410518

about

Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380)Antipsychotic-like effect of the muscarinic acetylcholine receptor agonist BuTAC in non-human primates Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents.Partial mGlu₅ Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects.Potentiation of M1 Muscarinic Receptor Reverses Plasticity Deficits and Negative and Cognitive Symptoms in a Schizophrenia Mouse Model.2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites.Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders.Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor.Disruption of the Na+ ion binding site as a mechanism for positive allosteric modulation of the mu-opioid receptor.Regulation of synaptic MAPK/ERK phosphorylation in the rat striatum and medial prefrontal cortex by dopamine and muscarinic acetylcholine receptors.Dopaminergic and cholinergic regulation of Fyn tyrosine kinase phosphorylation in the rat striatum in vivo.State-dependent alterations in sleep/wake architecture elicited by the M4 PAM VU0467154 - Relation to antipsychotic-like drug effects 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 Optimization of M4 positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology.Diverse Effects on M1 Signaling and Adverse Effect Liability within a Series of M1 Ago-PAMs.Allosteric Modulation of GPCRs: New Insights and Potential Utility for Treatment of Schizophrenia and Other CNS Disorders.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 Antipsychotic-like Effects of M4 Positive Allosteric Modulators Are Mediated by CB2 Receptor-Dependent Inhibition of Dopamine Release Cell-Type-Specific Translation Profiling Reveals a Novel Strategy for Treating Fragile X Syndrome.Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia.Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs.Pharmacological modulation of AMPA receptor phosphorylation by dopamine and muscarinic receptor agents in the rat medial prefrontal cortex.Prefrontal Cortex-Mediated Impairments in a Genetic Model of NMDA Receptor Hypofunction Are Reversed by the Novel M1 PAM VU6004256.Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping.Integrated regulation of AMPA glutamate receptor phosphorylation in the striatum by dopamine and acetylcholine.Discovery of a novel, CNS penetrant M4 PAM chemotype based on a 6-fluoro-4-(piperidin-1-yl)quinoline-3-carbonitrile core.In vivo neuroimaging and behavioral correlates in a rat model of chemotherapy-induced cognitive dysfunction.Positive allosteric modulation of M1 and M4 muscarinic receptors as potential therapeutic treatments for schizophrenia.The role of fMRI in drug development.Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides.Total RNA Sequencing of Rett Syndrome Autopsy Samples Identifies the M4 Muscarinic Receptor as a Novel Therapeutic Target.Brief exposure to obesogenic diet disrupts brain dopamine networks.Cholinergic Projections to the Substantia Nigra Pars Reticulata Inhibit Dopamine Modulation of Basal Ganglia through the M4 Muscarinic Receptor.

P2860

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P2860

Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100

http://www.wikidata.org/entity/Q30410518

description

2014 nî lūn-bûn

@nan

2014 թուականի Յունուարին հրատարակուած գիտական յօդուած

@hyw

2014 թվականի հունվարին հրատարակված գիտական հոդված

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2014年の論文

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2014年論文

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2014年論文

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2014年論文

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2014年論文

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2014年論文

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2014年论文

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name

Antipsychotic drug-like effect ...... allosteric modulator VU0152100

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Antipsychotic drug-like effect ...... allosteric modulator VU0152100

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Antipsychotic drug-like effect ...... allosteric modulator VU0152100

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Antipsychotic drug-like effect ...... allosteric modulator VU0152100

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Antipsychotic drug-like effect ...... allosteric modulator VU0152100

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Antipsychotic drug-like effect ...... allosteric modulator VU0152100

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Analisa Thompson

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Ariel Y Deutch

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Bruce J Melancon

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Carrie K Jones

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James C Tarr

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John Rosanelli

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John T Brogan

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Jürgen Wess

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Malcolm J Avison

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P2860

Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes

An allosteric enhancer of M₄ muscarinic acetylcholine receptor function inhibits behavioral and neurochemical effects of cocaine

A subpopulation of neuronal M4 muscarinic acetylcholine receptors plays a critical role in modulating dopamine-dependent behaviors

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

Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats

A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning

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

Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction

Identification of a family of muscarinic acetylcholine receptor genes

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

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10.1038/NPP.2014.2

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7

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39

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Craig W. Lindsley

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2014-01-20T00:00:00Z

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259808497

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