Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate recept
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Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenicsNeuroprotective and symptomatic effects of targeting group III mGlu receptors in neurodegenerative diseaseA novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites.Development of allosteric modulators of GPCRs for treatment of CNS disordersRadiosynthesis and evaluation of an 18F-labeled positron emission tomography (PET) radioligand for metabotropic glutamate receptor subtype 4 (mGlu4).Discovery, Synthesis, and Preclinical Characterization of N-(3-Chloro-4-fluorophenyl)-1H-pyrazolo[4,3-b]pyridin-3-amine (VU0418506), a Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 (mGlu4).Development and Antiparkinsonian Activity of VU0418506, a Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor 4 Homomers without Activity at mGlu2/4 Heteromers.Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability.The metabotropic glutamate receptor 8 agonist (S)-3,4-DCPG reverses motor deficits in prolonged but not acute models of Parkinson's disease.The Metabotropic Glutamate Receptor 4 Positive Allosteric Modulator ADX88178 Inhibits Inflammatory Responses in Primary MicrogliaPractical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate ReceptorsRecent advances in the drug discovery of metabotropic glutamate receptor 4 (mGluR4) activators for the treatment of CNS and non-CNS disorders.Metabotropic glutamate receptor 4 (mGlu4)-positive allosteric modulators for the treatment of Parkinson's disease: historical perspective and review of the patent literature.Targeting glutamate receptors to tackle the pathogenesis, clinical symptoms and levodopa-induced dyskinesia associated with Parkinson's disease.Therapeutic potential of targeting glutamate receptors in Parkinson's disease.Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core.Current Nondopaminergic Therapeutic Options for Motor Symptoms of Parkinson's Disease.Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool.Irreversible endo-selective diels-alder reactions of substituted alkoxyfurans: a general synthesis of endo-cantharimides.Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogsDevelopment 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 TypeSynthesis and evaluation of N-(methylthiophenyl)picolinamide derivatives as PET radioligands for metabotropic glutamate receptor subtype 4.Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy.Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4).In silico studies targeting G-protein coupled receptors for drug research against Parkinson's disease.
P2860
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P2860
Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate recept
description
2011 nî lūn-bûn
@nan
2011年の論文
@ja
2011年論文
@yue
2011年論文
@zh-hant
2011年論文
@zh-hk
2011年論文
@zh-mo
2011年論文
@zh-tw
2011年论文
@wuu
2011年论文
@zh
2011年论文
@zh-cn
name
Discovery, synthesis, and stru ...... metabotropic glutamate recept
@ast
Discovery, synthesis, and stru ...... metabotropic glutamate recept
@en
type
label
Discovery, synthesis, and stru ...... metabotropic glutamate recept
@ast
Discovery, synthesis, and stru ...... metabotropic glutamate recept
@en
prefLabel
Discovery, synthesis, and stru ...... metabotropic glutamate recept
@ast
Discovery, synthesis, and stru ...... metabotropic glutamate recept
@en
P2093
P2860
P50
P356
P1476
Discovery, synthesis, and stru ...... metabotropic glutamate recept
@en
P2093
Analisa D Thompson
Anna L Blobaum
C David Weaver
Carrie K Jones
Corey R Hopkins
Darren W Engers
J Scott Daniels
Jim Bogenpohl
Julie R Field
Rocco D Gogliotti
P2860
P304
P356
10.1021/JM200956Q
P407
P577
2011-10-19T00:00:00Z