43 articles for thisTarget
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Design and Synthesis of a Series of l-trans-4-Substituted Prolines as Selective Antagonists for the Ionotropic Glutamate Receptors Including Functional and X-ray Crystallographic Studies of New Subtype Selective Kainic Acid Receptor Subtype 1 (GluK1) Antagonist (2S,4R)-4-(2-Carboxyphenoxy)pyrrolidin
Mcgill University
Design, synthesis and structure-activity relationships of novel phenylalanine-based amino acids as kainate receptors ligands.
Jagiellonian University Medical College
Tweaking Subtype Selectivity and Agonist Efficacy at (S)-2-Amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propionic acid (AMPA) Receptors in a Small Series of BnTetAMPA Analogues.
University of Copenhagen
Studies on Aryl-Substituted Phenylalanines: Synthesis, Activity, and Different Binding Modes at AMPA Receptors.
University of Copenhagen
Structural studies, homology modeling and molecular docking of novel non-competitive antagonists of GluK1/GluK2 receptors.
Medical University of Lublin
Chemoenzymatic synthesis of new 2,4-syn-functionalized (S)-glutamate analogues and structure-activity relationship studies at ionotropic glutamate receptors and excitatory amino acid transporters.
University of Copenhagen
4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological characterization at ionotropic glutamate receptors of compounds related to glutamate and its homologues.
University of Turin
The glutamate receptor GluR5 agonist (S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid and the 8-methyl analogue: synthesis, molecular pharmacology, and biostructural characterization.
University of Copenhagen
1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of potent and Selective iGluR5 modulators.
European Research Centre For Drug Discovery and Development (Natsyndrugs)
Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7.
Universite Blaise Pascal
Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2.
Universite Blaise Pascal
Structures of the ligand-binding core of iGluR2 in complex with the agonists (R)- and (S)-2-amino-3-(4-hydroxy-1,2,5-thiadiazol-3-yl)propionic acid explain their unusual equipotency.
University of Copenhagen
Synthesis and pharmacological characterization at glutamate receptors of the four enantiopure isomers of tricholomic acid.
University of Milan
Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists.
University Walk
Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors.
University Walk
Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso-quinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine.
Eli Lilly
Piperazine-2,3-dicarboxylic acid derivatives as dual antagonists of NMDA and GluK1-containing kainate receptors.
University of Bristol
Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization.
University of Copenhagen
Biostructural and Pharmacological Studies of Bicyclic Analogues of the 3-Isoxazolol Glutamate Receptor Agonist Ibotenic Acid
TBA
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
Novartis Pharma
Domoic Acid as a Lead for the Discovery of the First Selective Ligand for Kainate Receptor Subtype 5 (GluK5).
University of Copenhagen
A tetrazolyl-substituted subtype-selective AMPA receptor agonist.
University of Copenhagen
Structure-activity relationship studies on N3-substituted willardiine derivatives acting as AMPA or kainate receptor antagonists.
University Walk
Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain.
Eli Lilly
Convergent synthesis and pharmacology of substituted tetrazolyl-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid analogues.
The Danish University of Pharmaceutical Sciences
Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.
Central South University
Bioisosteric modifications of 2-arylureidobenzoic acids: selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5.
The Danish University of Pharmaceutical Sciences
2-arylureidobenzoic acids: selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5.
The Danish University of Pharmaceutical Sciences
Design, synthesis, and pharmacology of a highly subtype-selective GluR1/2 agonist, (RS)-2-amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)propionic acid (Cl-HIBO).
The Danish University of Pharmaceutical Sciences
Pyrrolylquinoxalinediones carrying a piperazine residue represent highly potent and selective ligands to the homomeric kainate receptor GluR5.
Abbott
4-Alkyl- and 4-cinnamylglutamic acid analogues are potent GluR5 kainate receptor agonists.
Eli Lilly
Synthesis of a series of aryl kainic acid analogs and evaluation in cells stably expressing the kainate receptor humGluR6.
Eli Lilly
Allosteric control of an ionotropic glutamate receptor with an optical switch.
University of California Berkeley
( S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements and Structural and Biological Investigation.
University of Siena
Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist.
University of Eastern Finland
Molecular design and biological activity of potent and selective protein kinase inhibitors related to balanol.
University of California San Diego
Achiral oligoamines as versatile tool for the development of aspartic protease inhibitors.
Philipps University Marburg