Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS - Wikidata - wikimedia - TriplyDB

Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS

Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS

http://www.wikidata.org/entity/Q38539175

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Substituted 1-Phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction.(3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology.3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats.Fragile X syndrome: an update on developing treatment modalities.Recent advances in the design and development of novel negative allosteric modulators of mGlu(5)Parkinson's disease therapeutics: new developments and challenges since the introduction of levodopa."Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology.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 VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover.Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.

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P2860

Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS

http://www.wikidata.org/entity/Q38539175

description

2009 nî lūn-bûn

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2009年の論文

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2009年論文

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2009年論文

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2009年論文

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2009年論文

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2009年論文

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2009年论文

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2009年论文

@zh

2009年论文

@zh-cn

name

Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS

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type

label

Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS

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prefLabel

Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS

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J.BMCL.2009.10.059

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Bioorganic & Medicinal Chemistry Letters

P1476

Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS

@en

P2093

Alice L Rodriguez

http://www.w3.org/2001/XMLSchema#string

C David Weaver

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Richard Williams

http://www.w3.org/2001/XMLSchema#string

Ya Zhou

http://www.w3.org/2001/XMLSchema#string

P2860

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

Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists

Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity

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

Pharmacology and functions of metabotropic glutamate receptors

Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonist

Development of a custom high-throughput preparative liquid chromatography/mass spectrometer platform for the preparative purification and analytical analysis of compound libraries.

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.

Expedited SAR study of an mGluR5 antagonists: generation of a focused library using a solution-phase Suzuki coupling methodology.

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

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10.1016/J.BMCL.2009.10.059

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Craig W. Lindsley

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38053767

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19875287

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3177597

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