65 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
Organization
Development and SAR of functionally selective allosteric modulators of GABAA receptors.
Astrazeneca
Allyl m-trifluoromethyldiazirine mephobarbital: an unusually potent enantioselective and photoreactive barbiturate general anesthetic.
Massachusetts General Hospital
Discovery of the imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepine scaffold as a novel, potent and selective GABA(A) alpha5 inverse agonist series.
F. Hoffmann-La Roche
Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators.
University of California
4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships.
University of Copenhagen
Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders.
Merck Sharp Laboratory
Alpha-amino acid phenolic ester derivatives: novel water-soluble general anesthetic agents which allosterically modulate GABA(A) receptors.
Organon Research and Development Group
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.
University of Wisconsin-Milwaukee
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.
Merck
Triazoloquinazolinediones as novel high affinity ligands for the benzodiazepine site of GABA(A) receptors.
Lund University
Developing dual functional allosteric modulators of GABA(A) receptors.
Astrazeneca Pharmaceuticals
The GABA(A) receptor as a target for photochromic molecules.
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.
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.
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.
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.
Shimane University
Multiparameter Optimization of Naphthyridine Derivatives as Selective ?5-GABA
Gedeon Richter
2,3,7-Trisubstituted pyrazolo[1,5-d][1,2,4]triazines: functionally selective GABAA alpha3-subtype agonists.
Merck Sharp and Dohme Research Laboratories
A pyridazine series of alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.
Merck Sharp & Dohme Research Laboratories
Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology.
The Danish University of Pharmaceutical Sciences
Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety.
TBA
Imidazo[1,2-a]pyrimidines as functionally selective GABA(A) ligands.
Merck Sharp and Dohme Research Laboratories
8-Fluoroimidazo[1,2-a]pyridine: synthesis, physicochemical properties and evaluation as a bioisosteric replacement for imidazo[1,2-a]pyrimidine in an allosteric modulator ligand of the GABA A receptor.
Merck Sharp and Dohme Research Laboratories
Imidazo[1,2-b][1,2,4]triazines as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.
Merck Sharp and Dohme Research Laboratories
Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.
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.
Merck Sharp and Dohme Research Laboratories
A new pyridazine series of GABAA alpha5 ligands.
Merck Sharp & Dohme Research Laboratories
Pyrazolopyridinones as functionally selective GABAA ligands.
Merck Sharp & 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.
Merck Sharp & Dohme Research Laboratories
Structure-Activity Studies of 3,9-Diazaspiro[5.5]undecane-Based ?-Aminobutyric Acid Type A Receptor Antagonists with Immunomodulatory Effect.
University of Copenhagen
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.
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.
Merck Sharp and Dohme Research Laboratories
Neuroactive Type-A ?-Aminobutyric Acid Receptor Allosteric Modulator Steroids from the Hypobranchial Gland of Marine Mollusk,
University of Utah
2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor.
Merck Sharp & Dohme Research Laboratories
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.
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.
Merck Sharp and Dohme Research Laboratories
Tricyclic pyridones as functionally selective human GABAA alpha 2/3 receptor-ion channel ligands.
The Neuroscience Research Centre
Determination of the stable conformation of GABA(A)-benzodiazepine receptor bivalent ligands by low temperature NMR and X-ray analysis.
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.
University of Wisconsin-Milwaukee
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.
Merck Sharp & Dohme Research Laboratories
Discovery of ONO-8590580: A novel, potent and selective GABA
Charles River Discovery Research Services
3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.
Merck Sharp & Dohme Research Laboratories
A potent photoreactive general anesthetic with novel binding site selectivity for GABA
University of Illinois At Chicago
6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.
Merck Sharp & Dohme Research Laboratories
Fipronil-based photoaffinity probe for Drosophila and human beta 3 GABA receptors.
University of California
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.
The Royal Danish School of Pharmacy
N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit.
Merck Sharp & Dohme Research Laboratories
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.
University of Wisconsin-Milwaukee
GABA allosteric modulators: An overview of recent developments in non-benzodiazepine modulators.
The University of Sydney
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 receptors
University of Wisconsin-Milwaukee
Design, Synthesis, and Pharmacological Evaluation of Novel ?2/3 Subunit-Selective ?-Aminobutyric Acid Type A (GABA
University of Vienna
Efficient modulation of ?-aminobutyric acid type A receptors by piperine derivatives.
University of Vienna
Identification of dihydrostilbenes in Pholidota chinensis as a new scaffold for GABAA receptor modulators.
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.
Universit£
Progress in the discovery of small molecule modulators of the Cys-loop superfamily receptors.
Amgen
Discovery of the first low-shift positive allosteric modulators for the muscarinic M1 receptor.
Roche Pharma Research and Early Development
Synthesis and pharmacological evaluation of neurosteroid photoaffinity ligands.
University of Illinois At Chicago
Synthesis and Characterization of a Novel?-Aminobutyric Acid Type A (GABA
University of Wisconsin-Milwaukee
Neuroactive Steroids. 2. 3?-Hydroxy-3?-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5?-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (?-Aminobutyric Acid)
Sage Therapeutics
