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57 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists.EBI
University Of Copenhagen
Ion channels as therapeutic targets: a drug discovery perspective.EBI
Pfizer
Synthesis, pharmacological studies and molecular modeling of some tetracyclic 1,3-diazepinium chlorides.EBI
University Of The West Indies
Development and SAR of functionally selective allosteric modulators of GABAA receptors.EBI
Astrazeneca
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.EBI
Moltech
Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators.EBI
University Of California
Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders.EBI
Merck Sharp Laboratory
Synthesis, structure-activity relationships at the GABA(A) receptor in rat brain, and differential electrophysiological profile at the recombinant human GABA(A) receptor of a series of substituted 1,2-diphenylimidazoles.EBI
Universit£
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.EBI
University Of Wisconsin-Milwaukee
Synthesis and binding affinity of 2-phenylimidazo[1,2-alpha]pyridine derivatives for both central and peripheral benzodiazepine receptors. A new series of high-affinity and selective ligands for the peripheral type.EBI
Universit£
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.EBI
Merck
Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABAA receptor.EBI
Novartis Institutes For Biomedical Research
Triazoloquinazolinediones as novel high affinity ligands for the benzodiazepine site of GABA(A) receptors.EBI
Lund University
Developing dual functional allosteric modulators of GABA(A) receptors.EBI
Astrazeneca Pharmaceuticals
The GABA(A) receptor as a target for photochromic molecules.EBI
University Of Massachusetts
Design, synthesis, and subtype selectivity of 3,6-disubstitutedß-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.EBI
University Of Wisconsin-Milwaukee
The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction.EBI
F. Hoffmann-La Roche
Imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepines as potent and highly selective GABAA alpha5 inverse agonists with potential for the treatment of cognitive dysfunction.EBI
F. Hoffmann-La Roche
Synthesis, 3D-QSAR, and docking studies of 1-phenyl-1H-1,2,3-triazoles as selective antagonists for beta3 over alpha1beta2gamma2 GABA receptors.EBI
Shimane University
A pyridazine series of alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.EBI
Merck Sharp & Dohme Research Laboratories
Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety.EBI
TBA
Imidazo[1,2-b][1,2,4]triazines as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.EBI
Merck Sharp And Dohme Research Laboratories
7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models.EBI
Merck Sharp And Dohme Research Laboratories
Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit.EBI
Merck Sharp & Dohme Research Laboratories
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.EBI
Merck Sharp & Dohme Research Laboratories
Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site.EBI
Merck Sharp And Dohme Research Laboratories
2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor.EBI
Merck Sharp & Dohme Research Laboratories
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.EBI
Merck Sharp And Dohme Research Laboratories
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.EBI
Merck Sharp And Dohme Research Laboratories
Tricyclic pyridones as functionally selective human GABAA alpha 2/3 receptor-ion channel ligands.EBI
The Neuroscience Research Centre
Determination of the stable conformation of GABA(A)-benzodiazepine receptor bivalent ligands by low temperature NMR and X-ray analysis.EBI
University Of Wisconsin-Milwaukee
Synthesis, in vitro affinity, and efficacy of a bis 8-ethynyl-4H-imidazo[1,5a]- [1,4]benzodiazepine analogue, the first bivalent alpha5 subtype selective BzR/GABA(A) antagonist.EBI
University Of Wisconsin-Milwaukee
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.EBI
Merck Sharp & Dohme Research Laboratories
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.EBI
Neurogen
3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.EBI
Merck Sharp & Dohme Research Laboratories
6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.EBI
Merck Sharp & Dohme Research Laboratories
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.EBI
The Royal Danish School Of Pharmacy
N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit.EBI
Merck Sharp & Dohme Research Laboratories
Subtype Selective ?-Aminobutyric Acid Type A Receptor (GABAEBI
University Of Sussex
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via comparative molecular field analysis.EBI
University Of Wisconsin-Milwaukee
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) at wild type and recombinant GABAA receptorsEBI
University Of Wisconsin-Milwaukee
Synthesis and pharmacological properties of novel 8-substituted imidazobenzodiazepines: high-affinity, selective probes for alpha 5-containing GABAA receptors.EBI
University Of Wisconsin-Milwaukee
Efficient modulation of ?-aminobutyric acid type A receptors by piperine derivatives.EBI
University Of Vienna
Identification of dihydrostilbenes in Pholidota chinensis as a new scaffold for GABAA receptor modulators.EBI
University Of Basel
New insight into the central benzodiazepine receptor-ligand interactions: design, synthesis, biological evaluation, and molecular modeling of 3-substituted 6-phenyl-4H-imidazo[1,5-a][1,4]benzodiazepines and related compounds.EBI
Universit£
Progress in the discovery of small molecule modulators of the Cys-loop superfamily receptors.EBI
Amgen
Optimization of novel monobactams with activity against carbapenem-resistant Enterobacteriaceae - Identification of LYS228.EBI
Novartis Institutes For Biomedical Research
Discovery of the first low-shift positive allosteric modulators for the muscarinic M1 receptor.EBI
Roche Pharma Research And Early Development
Synthesis and Characterization of a Novel?-Aminobutyric Acid Type A (GABAEBI
University Of Wisconsin-Milwaukee
The amylase inhibitor montbretin A reveals a new glycosidase inhibition motif.BDB
University Of British Columbia
Structure-guided design of a high affinity inhibitor to human CtBP.BDB
University Of Massachusetts Medical School