43 articles for thisTarget
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Article Title
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Discovery of the Firsta-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP)¿-8.

Eli Lilly
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
Structure-activity relationship studies of N-methylated and N-hydroxylated spider polyamine toxins as inhibitors of ionotropic glutamate receptors.

University of Copenhagen
Ion channels as therapeutic targets: a drug discovery perspective.

Pfizer
Structure-activity relationship studies of argiotoxins: selective and potent inhibitors of ionotropic glutamate receptors.

University of Copenhagen
General synthesis ofß-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ionotropic glutamate receptors.

University of Copenhagen
Solid-phase synthesis and biological evaluation of Joro spider toxin-4 from Nephila clavata.

University of Copenhagen
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)
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
Functional characterization of Tet-AMPA [tetrazolyl-2-amino-3-(3-hydroxy-5-methyl- 4-isoxazolyl)propionic acid] analogues at ionotropic glutamate receptors GluR1-GluR4. The molecular basis for the functional selectivity profile of 2-Bn-Tet-AMPA.

University of Copenhagen
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.

University of Urbino
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
Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes.

University of Bristol
(R)-4-oxo-5-phosphononorvaline: a new competitive glutamate antagonist at the NMDA receptor complex.

Merrell Dow Research Institute
4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists.

Eli Lilly
A new phenylalanine derivative acts as an antagonist at the AMPA receptor GluA2 and introduces partial domain closure: synthesis, resolution, pharmacology, and crystal structure.

University of Copenhagen
Biostructural and Pharmacological Studies of Bicyclic Analogues of the 3-Isoxazolol Glutamate Receptor Agonist Ibotenic Acid

TBA
Positive allosteric modulators of thea-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor.

Merck Research Laboratories
Quinazolin-4-one derivatives: A novel class of noncompetitive NR2C/D subunit-selective N-methyl-D-aspartate receptor antagonists.

Emory University
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.

Novartis Pharma
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.

University of California
Synthesis and biology of the rigidified glutamate analogue,
trans-2-carboxyazetidine-3-acetic acid (
t-CAA)

TBA
A tetrazolyl-substituted subtype-selective AMPA receptor agonist.

University of Copenhagen
Uncompetitive antagonism of AMPA receptors: Mechanistic insights from studies of polyamine toxin derivatives.

The Danish University of Pharmaceutical Sciences
Structure-activity relationship studies on N3-substituted willardiine derivatives acting as AMPA or kainate receptor antagonists.

University Walk
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
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
(S)-2-Amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid, a potent and selective agonist at the GluR5 subtype of ionotropic glutamate receptors. Synthesis, modeling, and molecular pharmacology.

The Danish University of Pharmaceutical Sciences
Solid-phase synthesis of polyamine toxin analogues: potent and selective antagonists of Ca2+-permeable AMPA receptors.

The Royal Danish School of Pharmacy
Characterization of the 1H-cyclopentapyrimidine-2,4(1H,3H)-dione derivative (S)-CPW399 as a novel, potent, and subtype-selective AMPA receptor full agonist with partial desensitization properties.

Universita' Degli Studi Di Siena
4-Alkyl- and 4-cinnamylglutamic acid analogues are potent GluR5 kainate receptor agonists.

Eli Lilly
Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands.

University of Turin
Synthesis, resolution, and biological evaluation of the four stereoisomers of 4-methylglutamic acid: selective probes of kainate receptors.

Symphony Pharmaceuticals
Controlling Ca

University of Copenhagen
Development of novel N-3-bromoisoxazolin-5-yl substituted 2,3-benzodiazepines as noncompetitive AMPAR antagonists.

University of Messina
LSD1 inhibitors and medical uses thereof

Constellation Pharmaceuticals
Hexahydropyrroloimidazolone compounds

Hoffmann-La Roche