136 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
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The Structure-Activity Relationship of a Tetrahydroisoquinoline Class of N-Methyl-d-Aspartate Receptor Modulators that Potentiates GluN2B-Containing N-Methyl-d-Aspartate Receptors.
Emory University
Systematic variation of the benzenesulfonamide part of the GluN2A selective NMDA receptor antagonist TCN-201.
University of M£Nster
Unusual synthesis of new glycine antagonists via sequential aldol condensation-lactonization-elimination reaction.
Glaxowellcome
Neurosteroid-like Inhibitors of N-Methyl-d-aspartate Receptor: Substituted 2-Sulfates and 2-Hemisuccinates of Perhydrophenanthrene.
Academy of Sciences of The Czech Republic
A novel class of negative allosteric modulators of NMDA receptor function.
Emory University
Structure-activity relationship studies of N-methylated and N-hydroxylated spider polyamine toxins as inhibitors of ionotropic glutamate receptors.
University of Copenhagen
Design, synthesis, and structure-activity relationship of a novel series of GluN2C-selective potentiators.
Emory University
Synthesis and structure activity relationship of tetrahydroisoquinoline-based potentiators of GluN2C and GluN2D containing N-methyl-D-aspartate receptors.
Emory University
Development of 2'-substituted (2S,1'R,2'S)-2-(carboxycyclopropyl)glycine analogues as potent N-methyl-d-aspartic acid receptor agonists.
University of Copenhagen
Structure-activity relationship studies of argiotoxins: selective and potent inhibitors of ionotropic glutamate receptors.
University of Copenhagen
Synthesis and biological characterization of 3-substituted 1H-indoles as ligands of GluN2B-containing N-methyl-D-aspartate receptors. Part 2.
University of Messina
Solid-phase synthesis and biological evaluation of Joro spider toxin-4 from Nephila clavata.
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
Enantiomeric propanolamines as selective N-methyl-D-aspartate 2B receptor antagonists.
Emory University
N-Hydroxypyrazolyl glycine derivatives as selective N-methyl-D-aspartic acid receptor ligands.
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
Synthesis of N-substituted 4-(4-hydroxyphenyl)piperidines, 4-(4-hydroxybenzyl)piperidines, and (+/-)-3-(4-hydroxyphenyl)pyrrolidines: selective antagonists at the 1A/2B NMDA receptor subtype.
Cocensys
Design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine sigma ligands as potential antipsychotic drugs.
Taisho Pharmaceutical
Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.
University of Oregon
Synthesis of 1,4,7,8,9,10-hexahydro-9-methyl-6-nitropyrido[3,4-f]- quinoxaline-2,3-dione and related quinoxalinediones: characterization of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (and N-methyl-D-aspartate) receptor and anticonvulsant activity.
Warner-Lambert
Synthesis and excitatory amino acid pharmacology of a series of heterocyclic-fused quinoxalinones and quinazolinones.
Eli Lilly
Synthesis and structure-activity relationship of C5-substituted analogues of (+-)-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine [(+-)-desmethyl-MK801]: ligands for the NMDA receptor-coupled phencyclidine binding site.
National Institute of Diabetes and Digestive and Kidney Diseases
5-Aminomethylquinoxaline-2,3-diones, Part III: Arylamide derivatives as highly potent and selective glycine-site NMDA receptor antagonists.
Novartis Pharma
5-Aminomethylquinoxaline-2,3-diones. Part I: A novel class of AMPA receptor antagonists.
Novartis Pharma
Synthesis and glutamate antagonist activity of 4-phosphonoalkylquinoline derivatives: A novel class of non-NMDA antagonist
TBA
Piperazine-2,3-dicarboxylic acid derivatives as dual antagonists of NMDA and GluK1-containing kainate receptors.
University of Bristol
Quinazolin-4-one derivatives: A novel class of noncompetitive NR2C/D subunit-selective N-methyl-D-aspartate receptor antagonists.
Emory University
Synthesis, structural activity-relationships, and biological evaluation of novel amide-based allosteric binding site antagonists in NR1A/NR2B N-methyl-D-aspartate receptors.
Emory University
3-(aminomethyl)piperazine-2,5-dione as a novel NMDA glycine site inhibitor from the chemical universe database GDB.
University of Berne
6,7,8,9-tetrahydro-3-hydroxy-1H-1-benzazepine-2,5-diones via a diels-alder reaction:antagonists with a non-planar hydrophobic region for NMDA receptor glycine sites
TBA
Structure-activity relationships of tricyclic quinoxalinediones as potent antagonists for the glycine binding site of the NMDA receptor 2
TBA
Structure-activity relationships of tricyclic quinoxalinediones as potent antagonists for the glycine binding site of the NMDA receptor 1
TBA
NS 257 (1,2,3,6,7,8-hexahydro-3(hydroxyimino)-N,N,7-trimethyl-2-oxobenzo[2,1-b:3,4-c']dipyrrole-5-sulfonamide) is a potent, systemically active ampa receptor antagonist
TBA
Structure-activity relationships of a series of glycine antagonists related to 5,7-dichlorokynurenic acid and 3-(2-carboxy-6-chloroindol-3-yl)acetic acid
TBA
Derivatives of 1-hydroxy-3-aminopyrrolidin-2-one (HA-966). Partial agonists at the glycine site of the NMDA receptor
TBA
2-carboxy indolines and indoles as potential glycine/NMDA antagonists: effect of five-membered ring conformation on affinity.
TBA
Design, synthesis and molecular modeling of 3-acylamino-2- Carboxyindole NMDA receptor glycine-site antagonists
TBA
Design and synthesis of indole-based peptoids as potent noncompetitive antagonists of transient receptor potential vanilloid 1.
University of Barcelona
Synthesis and biological evaluation of 1-amino-2-phosphonomethylcyclopropanecarboxylic acids, new group III metabotropic glutamate receptor agonists.
University Paris Descartes
Design, synthesis, and in vitro and in vivo characterization of new memantine analogs for Alzheimer's disease.
Universitat De Barcelona
NMDA-NR2B subtype selectivity of stereoisomeric 2-(1,2,3,4-tetrahydro-1-isoquinolyl)ethanol derivatives.
Ludwig-Maximilians-UniversitäT MüNchen
Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists.
University Walk
3-hydroxy-quinazoline-2,4-dione as a useful scaffold to obtain selective Gly/NMDA and AMPA receptor antagonists.
Universita Degli Studi Di Firenze
Subtype selective NMDA receptor antagonists: evaluation of some novel alkynyl analogues.
Pfizer
Synthesis and biological evaluation of analogues of 7-chloro-4,5-dihydro-4- oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid (TQX-173) as novel selective AMPA receptor antagonists.
Universita Degli Studi Di Firenze
Selectivity fields: comparative molecular field analysis (CoMFA) of the glycine/NMDA and AMPA receptors.
Moscow State University
Tricyclic indole-2-carboxylic acids: highly in vivo active and selective antagonists for the glycine binding site of the NMDA receptor.
Sumitomo Pharmaceuticals
Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists.
Università
Synthesis and biological evaluation of a new set of pyrazolo[1,5-c]quinazoline-2-carboxylates as novel excitatory amino acid antagonists.
Universita' Di Firenze
Investigation of the structural requirements for N-methyl-D-aspartate receptor positive and negative allosteric modulators based on 2-naphthoic acid.
University of Bristol
Evaluation and biological properties of reactive ligands for the mapping of the glycine site on the N-methyl-D-aspartate (NMDA) receptor.
Université
Discovery of subtype-selective NMDA receptor ligands: 4-benzyl-1-piperidinylalkynylpyrroles, pyrazoles and imidazoles as NR1A/2B antagonists.
Warner-Lambert
Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.
University of Oregon
4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist.
Cocensys
4,5-Dihydro-1,2,4-triazolo[1,5-a]quinoxalin-4-ones: excitatory amino acid antagonists with combined glycine/NMDA and AMPA receptor affinity.
Universita' Di Firenze
Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(arylalkynyl)-4-benzylpiperidines.
Cocensys
Structure-activity relationship for a series of 2-substituted 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indoles: potent subtype-selective inhibitors of N-methyl-D-aspartate (NMDA) receptors.
University of Oregon
Design, synthesis and structure-activity relationships of novel strychnine-insensitive glycine receptor ligands.
Institut De Recherches Servier
Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands.
University of Turin
Di-aryl Sulfonamide Motif Adds π-Stacking Bulk in Negative Allosteric Modulators of the NMDA Receptor.
Emory University
(E)-3-(2-(N-phenylcarbamoyl)vinyl)pyrrole-2-carboxylic acid derivatives. A novel class of glycine site antagonists.
Università
5-(N-oxyaza)-7-substituted-1,4-dihydroquinoxaline-2,3-diones: novel, systemically active and broad spectrum antagonists for NMDA/glycine, AMPA, and kainate receptors.
Cocensys
Synthesis of racemic 6,7,8,9-tetrahydro-3-hydroxy-1H-1-benzazepine-2,5-diones as antagonists of N-methyl-d-aspartate (NMDA) and alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptors.
Cocensys
4-substituted-3-phenylquinolin-2(1H)-ones: acidic and nonacidic glycine site N-methyl-D-aspartate antagonists with in vivo activity.
Merck Sharp and Dohme Research Laboratories
Structure-activity relationships of alkyl- and alkoxy-substituted 1,4-dihydroquinoxaline-2,3-diones: potent and systemically active antagonists for the glycine site of the NMDA receptor.
Cocensys
Novel AMPA receptor antagonists: synthesis and structure-activity relationships of 1-hydroxy-7-(1H-imidazol-1-yl)-6-nitro-2,3(1H,4H)- quinoxalinedione and related compounds.
Yamanouchi Pharmaceutical
Synthesis and structure-activity relationships of 1,2,3,4-tetrahydroquinoline-2,3,4-trione 3-oximes: novel and highly potent antagonists for NMDA receptor glycine site.
Cocensys
Novel alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate receptor antagonists: synthesis and structure-activity relationships of 6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-pyrido[2,3-b]pyrazinedione and related compounds.
Yamanouchi Pharmaceutical
3-Nitro-3,4-dihydro-2(1H)-quinolones. Excitatory amino acid antagonists acting at glycine-site NMDA and (RS)-alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors.
Merck Sharp and Dohme Research Laboratories
3'-(Arylmethyl)- and 3'-(aryloxy)-3-phenyl-4-hydroxyquinolin-2(1H)-ones: orally active antagonists of the glycine site on the NMDA receptor.
Merck Sharp and Dohme Research Laboratories
Identification of 3,5-dihydro-2-aryl-1H-pyrazolo[3,4-c]quinoline-1,4(2H)-diones as novel high-affinity glycine site N-methyl-D-aspartate antagonists.
Merck Sharp and Dohme Research Laboratories
Resolution, absolute stereochemistry, and pharmacology of the S-(+)- and R-(-)-isomers of the apparent partial AMPA receptor agonist (R,S)-2-amino-3-(3-hydroxy-5-phenylisoxazol-4-yl)propionic acid [(R,S)-APPA].
Royal Danish School of Pharmacy
Substituted indole-2-carboxylates as in vivo potent antagonists acting as the strychnine-insensitive glycine binding site.
Glaxo Wellcome
Positive Modulators of the N-Methyl-d-aspartate Receptor: Structure-Activity Relationship Study of Steroidal 3-Hemiesters.
Institute of Physiology of The Czech Academy of Sciences
Design, synthesis, and evaluation of polyamine-memantine hybrids as NMDA channel blockers.
Hiroshima University
Evaluation and synthesis of aminohydroxyisoxazoles and pyrazoles as potential glycine agonists.
Warner-Lambert
Synthesis, stereochemistry, and biological activity of the 1-(1-phenyl-2-methylcyclohexyl)piperidines and the 1-(1-phenyl-4-methylcyclohexyl)piperidines. Absolute configuration of the potent trans-(-)-1-(1-phenyl-2-methylcyclohexyl)piperidine.
Istituto Superiore Di Sanità
Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites.
University of Paris
4-Amido-2-carboxytetrahydroquinolines. Structure-activity relationships for antagonism at the glycine site of the NMDA receptor.
Merck Sharp and Dohme Research Laboratories
3-(2-Carboxyindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site.
Marion Merrell Dow Research Institute
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
Synthesis, configuration, and activity of isomeric 2-phenyl-2-(N-piperidinyl)bicyclo[3.1.0]hexanes at phencyclidine and sigma binding sites.
National Institute of Diabetes and Digestive and Kidney Diseases
3-Phenyl-4-hydroxyquinolin-2(1H)-ones: potent and selective antagonists at the strychnine-insensitive glycine site on the N-methyl-D-aspartate receptor complex.
Eli Lilly
Beta-proline analogues as agonists at the strychnine-sensitive glycine receptor.
Warner-Lambert
Spiro-lactam NMDA receptor modulators and uses thereof
Tenacia Biotechnology (Hong Kong) Co.
Dizocilpine derivatives as peripheral NMDA receptor antagonists
Institut National De La Sante Et De La Recherche Medicale (Inserm
Amantadine nitrate compounds with neural protective effect, and preparation and medical use thereof
TBA
Highly selective sigma receptor ligands and radioligands as probes in nociceptive processing and the pathphysiological study of memory deficits and cognitive disorders
The University of Mississippi
Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic stroke.
Taisho Pharmaceutical
Characterization of two novel N-methyl-D-aspartate antagonists: EAA-090 (2-[8,9-dioxo-2,6-diazabicyclo [5.2.0]non-1(7)-en2-yl]ethylphosphonic acid) and EAB-318 (R-alpha-amino-5-chloro-1-(phosphonomethyl)-1H-benzimidazole-2-propanoic acid hydrochloride).
Wyeth Research
Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology.
Case Western Reserve University
3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro.
Case Western Reserve University
N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties.
Pudue Pharma Discovery Research
L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists.
Case Western Reserve University
Anxiolytic-like and antidepressant-like activities of MCL0129 (1-[(S)-2-(4-fluorophenyl)-2-(4-isopropylpiperadin-1-yl)ethyl]-4-[4-(2-methoxynaphthalen-1-yl)butyl]piperazine), a novel and potent nonpeptide antagonist of the melanocortin-4 receptor.
Taisho Pharmaceutical
Atomoxetine increases extracellular levels of norepinephrine and dopamine in prefrontal cortex of rat: a potential mechanism for efficacy in attention deficit/hyperactivity disorder.
Eli Lilly
Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.
Case Western Reserve University
In vitro receptor screening of pure constituents of St. John's wort reveals novel interactions with a number of GPCRs.
WestfÄLische Wilhelms-UniversitÄ
Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors.
Eli Lilly
Resolution, configurational assignment, and enantiopharmacology at glutamate receptors of 2-amino-3-(3-carboxy-5-methyl-4-isoxazolyl)propionic acid (ACPA) and demethyl-ACPA.
The Royal Danish School of Pharmacy
The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor.
Case Western Reserve University
The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.
Janssen Research Foundation
Stereochemistry and molecular pharmacology of (S)-thio-ATPA, a new potent and selective GluR5 agonist.
The Royal Danish School of Pharmacy
ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.
Abbott Laboratories
Novel structure having antagonist actions at both the glycine site of the N-methyl-D-aspartate receptor and neuronal voltage-sensitive sodium channels: biochemical, electrophysiological, and behavioral characterization.
University of Colorado
In vitro binding properties in rat brain of [3H]Ro 25-6981, a potent and selective antagonist of NMDA receptors containing NR2B subunits.
F. Hoffmann-La Roche
DL-threo-beta-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters.
Suntory Institute For Bioorganic Research
The pharmacological characterization of a novel selective 5-hydroxytryptamine1A receptor antagonist, NAD-299.
Preclinical R & D, Astra Arcus
RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist.
Roche Bioscience
Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity.
SynthÉLabo Recherche
A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: in vitro pharmacological properties of a novel, high affinity alpha 4 beta 2 nicotinic acetylcholine receptor ligand.
Abbott Laboratories
Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed.
Vrije Universiteit
YM90K: pharmacological characterization as a selective and potent alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate/kainate receptor antagonist.
Yamanouchi Pharmaceutical
GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor.
Glaxo Group Research
RS 39604: a potent, selective and orally active 5-HT4 receptor antagonist.
Syntex Discovery Research
Different binding affinities of NMDA receptor channel blockers in various brain regions--indication of NMDA receptor heterogeneity.
Merz
(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: I. In vitro characterization.
Abbott Laboratories
Actions of phenylglycine analogs at subtypes of the metabotropic glutamate receptor family.
Novo Nordisk
Pharmacological and autoradiographic discrimination of sigma and phencyclidine receptor binding sites in brain with (+)-[3H]SKF 10,047, (+)-[3H]-3-[3-hydroxyphenyl]-N-(1-propyl)piperidine and [3H]-1-[1-(2-thienyl)cyclohexyl]piperidine.
The Johns Hopkins University
Displacement of DL-[3H]-2-amino-4-phosphonobutanoic acid ( [3H]APB) binding with methyl-substituted APB analogues and glutamate agonists.
University of Minnesota
Characterization of the binding of [3H]-CGS 19755: a novel N-methyl-D-aspartate antagonist with nanomolar affinity in rat brain.
Ciba-Geigy
NMDA receptor agonists derived from ibotenic acid. Preparation, neuroexcitation and neurotoxicity.
Royal Danish School of Pharmacy