(Q38162957)

30 August 2017

Metabotropic glutamate receptor 5-positive allosteric modulators for the treatment of schizophrenia (2004-2012). (English)

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30 August 2017

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Craig W Lindsley

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30 August 2017

Shaun R Stauffer

2

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30 August 2017

1 January 2013

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Pharmaceutical patent analyst

30 August 2017

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30 August 2017

2

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30 August 2017

1

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30 August 2017

93-108

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Contrasts between patients with affective disorders and patients with schizophrenia on a neuropsychological test battery.

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Cognitive impairments in patients with schizophrenia displaying preserved and compromised intellect.

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New possibilities in cognition enhancement for schizophrenia.

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The current status of the dopamine hypothesis of schizophrenia

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Schizophrenia: moving beyond monoamine antagonists

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Dopamine hypothesis of schizophrenia: making sense of it all.

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Metabotropic glutamate receptors as therapeutic targets for schizophrenia

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From revolution to evolution: the glutamate hypothesis of schizophrenia and its implication for treatment

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Progress towards validating the NMDA receptor hypofunction hypothesis of schizophrenia

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Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia

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Progress in the preparation and testing of glycine transporter type-1 (GlyT1) inhibitors

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Recent progress in the discovery of non-sarcosine based GlyT1 inhibitors

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Glycine transporter-1: a new potential therapeutic target for schizophrenia

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Glycine reuptake inhibitor RG1678: a pharmacologic characterization of an investigational agent for the treatment of schizophrenia

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Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders

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The antipsychotic potential of muscarinic allosteric modulation

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Discovery of positive allosteric modulators of metabotropic glutamate receptor subtype 5 (mGluR5).

21 January 2018

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Direct and indirect modulation of the N-methyl D-aspartate receptor

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Metabotropic glutamate receptors: potential drug targets for the treatment of schizophrenia

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Regulation of neurotransmitter release by metabotropic glutamate receptors

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Pharmacology and functions of metabotropic glutamate receptors

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Pharmacological agents acting at subtypes of metabotropic glutamate receptors

21 January 2018

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Progress toward positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).

21 January 2018

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When simple agonism is not enough: emerging modalities of GPCR ligands.

21 January 2018

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Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery

21 January 2018

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Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

21 January 2018

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Recent progress in the synthesis and characterization of group II metabotropic glutamate receptor allosteric modulators.

21 January 2018

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Recent progress on the identification of metabotropic glutamate 4 receptor ligands and their potential utility as CNS therapeutics

21 January 2018

1 reference

Metabotropic glutamate receptor 4 (mGlu4)-positive allosteric modulators for the treatment of Parkinson's disease: historical perspective and review of the patent literature

21 January 2018

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Allosteric modulation of kinases and GPCRs: design principles and structural diversity

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Allosteric modulation of G-protein coupled receptors.

21 January 2018

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Allosteric binding sites on cell-surface receptors: novel targets for drug discovery

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G-protein-coupled receptors: from classical modes of modulation to allosteric mechanisms

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Positive and negative allosteric modulation of metabotropic glutamate receptors: emerging therapeutic potential

21 January 2018

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"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology

21 January 2018

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Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold

21 January 2018

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Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines

21 January 2018

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Allosteric potentiators of metabotropic glutamate receptor subtype 5 have differential effects on different signaling pathways in cortical astrocytes

21 January 2018

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A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.

21 January 2018

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Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo

21 January 2018

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

21 January 2018

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Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.

21 January 2018

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A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain

21 January 2018

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Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology

21 January 2018

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ADX47273 [S-(4-fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl}-methanone]: a novel metabotropic glutamate receptor 5-selective positive allosteric modulator with preclinical antipsychotic-like and procognitive activiti

21 January 2018

1 reference

Synthesis, SAR and unanticipated pharmacological profiles of analogues of the mGluR5 ago-potentiator ADX-47273

21 January 2018

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Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists

21 January 2018

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Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function.

21 January 2018

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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

21 January 2018

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Positive allosteric modulation of mGluR5 receptors facilitates extinction of a cocaine contextual memory

21 January 2018

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Metabotropic glutamate receptor ligands as potential therapeutics for addiction

21 January 2018

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Dose-dependent effect of CDPPB, the mGluR5 positive allosteric modulator, on recognition memory is associated with GluR1 and CREB phosphorylation in the prefrontal cortex and hippocampus.

21 January 2018

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Differential effects of the mGluR5 positive allosteric modulator CDPPB in the cortex and striatum following repeated administration.

21 January 2018

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Selective remediation of reversal learning deficits in the neurodevelopmental MAM model of schizophrenia by a novel mGlu5 positive allosteric modulator

21 January 2018

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In vitro characterisation of the novel positive allosteric modulators of the mGlu₅ receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat.

21 January 2018

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The mGlu₅ positive allosteric modulator LSN2463359 differentially modulates motor, instrumental and cognitive effects of NMDA receptor antagonists in the rat.

21 January 2018

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Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold

21 January 2018

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Design and synthesis of substituted N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides as positive allosteric modulators of the metabotropic glutamate receptor subtype 5.

21 January 2018

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Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes

21 January 2018

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Positive and negative modulation of group I metabotropic glutamate receptors

21 January 2018

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Discovery of novel positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).

21 January 2018

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Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator.

21 January 2018

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Efficacy switching SAR of mGluR5 allosteric modulators: highly potent positive and negative modulators from one chemotype

21 January 2018

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Preclinical profile of a novel metabotropic glutamate receptor 5 positive allosteric modulator

21 January 2018

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Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover

21 January 2018

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Quantitative analysis reveals multiple mechanisms of allosteric modulation of the mGlu5 receptor in rat astroglia

21 January 2018

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Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships

21 January 2018

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Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity

21 January 2018

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4-aryl piperazine and piperidine amides as novel mGluR5 positive allosteric modulators

21 January 2018

1 reference

21 January 2018

Identifiers

DOI

10.4155/PPA.12.82

1 reference

30 August 2017

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PubMed ID

24236973