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

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

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

http://www.wikidata.org/entity/Q24626912

about

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.Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology.Identification of Metabotropic Glutamate Receptor Subtype 5 Potentiators Using Virtual High-Throughput Screening.Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM.Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009.Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu₅).Positive allosteric modulators of type 5 metabotropic glutamate receptors (mGluR5) and their therapeutic potential for the treatment of CNS disorders.Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery Progress toward positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5)."Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology.Metabotropic glutamate receptor 5-positive allosteric modulators for the treatment of schizophrenia (2004-2012).Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype.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.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.Metabotropic glutamate receptor 5 - a promising target in drug development and neuroimaging.Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold.Acyl-2-aminobenzimidazoles: a novel class of neuroprotective agents targeting mGluR5 Cyclopropyl-containing positive allosteric modulators of metabotropic glutamate receptor subtype 5.Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity.Potentiating mGluR5 function with a positive allosteric modulator enhances adaptive learning.Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors – A Structural Perspective of Ligands and Mutants.

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

http://www.wikidata.org/entity/Q24626912

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2009 nî lūn-bûn

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2009 թուականի Ապրիլին հրատարակուած գիտական յօդուած

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2009年論文

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2009年论文

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Single photon emission computerized tomography imaging of amphetamine-induced dopamine release in drug-free schizophrenic subjects

Positron emission tomographic analysis of central D1 and D2 dopamine receptor occupancy in patients treated with classical neuroleptics and clozapine. Relation to extrapyramidal side effects

2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist

Recent advances in the phencyclidine model of schizophrenia

Pharmacology and functions of metabotropic glutamate receptors

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.

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

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

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

Mechanisms of typical and atypical antipsychotic drug action in relation to dopamine and NMDA receptor hypofunction hypotheses of schizophrenia.

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