125 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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Synthesis and pharmacological evaluation of pyrazolo[1,5-a]pyrimidin-7(4H)-one derivatives as potential GABA
Universit£
Design, synthesis, and biological evaluation of fluorinated imidazo[1,2-a]pyridine derivatives with potential antipsychotic activity.
Jagiellonian University Medical College
Nitrogenated honokiol derivatives allosterically modulate GABAA receptors and act as strong partial agonists.
University of Graz
MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors.
Takeda Pharmaceutical
Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists.
University of Copenhagen
Synthesis of novel cognition enhancers with pyrazolo[5,1-c][1,2,4]benzotriazine core acting at¿-aminobutyric acid type A (GABA(A)) receptor.
Sintesi E Studio Di Eterocicli Biologicamente Attivi (Heterobiolab) Universit£
Synthesis, pharmacological studies and molecular modeling of some tetracyclic 1,3-diazepinium chlorides.
University of The West Indies
4D-QSAR analysis of a set of propofol analogues: mapping binding sites for an anesthetic phenol on the GABA(A) receptor.
University of Chicago Medical Center
Allyl m-trifluoromethyldiazirine mephobarbital: an unusually potent enantioselective and photoreactive barbiturate general anesthetic.
Massachusetts General Hospital
Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acid(A) receptor ligands: synthesis, pharmacology, and structure-activity relationships.
University of Copenhagen
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
Moltech
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
2-(3-Methyl-3H-diaziren-3-yl)ethyl 1-(1-phenylethyl)-1H-imidazole-5-carboxylate: a derivative of the stereoselective general anesthetic etomidate for photolabeling ligand-gated ion channels.
Massachusetts General Hospital
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
Synthesis and in vitro activity of 3 beta-substituted-3 alpha-hydroxypregnan-20-ones: allosteric modulators of the GABAA receptor.
Cocensys
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.
Merck
Modulation of GABAA-receptors by honokiol and derivatives: subtype selectivity and structure-activity relationship.
University of Vienna
Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABAA receptor.
Novartis Institutes For Biomedical Research
Novel Cyclic Phosphinic Acids as GABAC ρ Receptor Antagonists: Design, Synthesis, and Pharmacology
TBA
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
A conformational study of ligands for omega modulatory sites of GABAa receptors by NOESY NMR spectroscopy and distance geometry
TBA
Proximity-accelerated chemical coupling reaction in the benzodiazepine-binding site of gamma-aminobutyric acid type A receptors: superposition of different allosteric modulators.
University of Bern
Identification of anesthetic binding sites on human serum albumin using a novel etomidate photolabel.
Imperial College
Synthesis and evaluation in monkey of two sensitive 11C-labeled aryloxyanilide ligands for imaging brain peripheral benzodiazepine receptors in vivo.
National Institute of Mental Health
5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.
University of Copenhagen
Enaminone amides as novel orally active GABAA receptor modulators.
University of California Irvine
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
4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Lund University
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
Rationalizing the binding and ? subtype selectivity of synthesized imidazodiazepines and benzodiazepines at GABAA receptors by using molecular docking studies.
University of Wisconsin-Milwaukee
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
Pharmacological Analysis of the Anti-inflammatory and Antiallodynic Effects of Zinagrandinolide E from
Universidad Nacional Aut£Noma De M£Xico
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
Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors.
University of Sydney
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.
Merck Sharp & Dohme Research Laboratories
Synthesis and Biological Evaluation of Pyrroloindolines as Positive Allosteric Modulators of the ?1?2?2 GABA
California Institute of Technology
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.
Neurogen
A new chromanone derivative isolated from Hypericum lissophloeus (Hypericaceae) potentiates GABAA receptor currents in a subunit specific fashion.
University of Graz
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
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.
The Royal Danish School of Pharmacy
Discovery of 2-(Imidazo[1,2- b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the ?-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites.
University of Copenhagen
N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit.
Merck Sharp & Dohme Research Laboratories
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.
Palack£
Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at ?-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.
University of Copenhagen
1-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting d-alanine-d-alanine ligase in bacterio.
Universit£
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
Propofol analogues. Synthesis, relationships between structure and affinity at GABAA receptor in rat brain, and differential electrophysiological profile at recombinant human GABAA receptors.
Università
Synthesis and Biological Studies of (+)-Liquiditerpenoic Acid A (Abietopinoic Acid) and Representative Analogues: SAR Studies.
Universitat Polit£Cnica De Valencia-Consejo Superior De Investigaciones Cient£Ficas
3 alpha-Hydroxy-3 beta-(phenylethynyl)-5 beta-pregnan-20-ones: synthesis and pharmacological activity of neuroactive steroids with high affinity for GABAA receptors.
Cocensys
Discovery of [1,2,4]-triazolo [1,5-a]pyrimidine-7(4H)-one derivatives as positive modulators of GABA
Qingdao University of Science and Technology
Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic ?-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.
Northwest University
Design, Synthesis, and Pharmacological Evaluation of Novel ?2/3 Subunit-Selective ?-Aminobutyric Acid Type A (GABA
University of Vienna
Synthesis and pharmacological properties of novel 8-substituted imidazobenzodiazepines: high-affinity, selective probes for alpha 5-containing GABAA receptors.
University of Wisconsin-Milwaukee
High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex.
Upjohn Laboratories
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
Exploring the orthosteric binding site of the ?-aminobutyric acid type A receptor using 4-(Piperidin-4-yl)-1-hydroxypyrazoles 3- or 5-imidazolyl substituted: design, synthesis, and pharmacological evaluation.
University of Copenhagen
Synthesis and evaluation of highly potent GABA(A) receptor antagonists based on gabazine (SR-95531).
University College London
p-Trifluoromethyldiazirinyl-etomidate: a potent photoreactive general anesthetic derivative of etomidate that is selective for ligand-gated cationic ion channels.
Massachusetts General Hospital
Synthesis and biological evaluation of flavan-3-ol derivatives as positive modulators of GABAA receptors.
The University of Sydney
Affinity of 3-acyl substituted 4-quinolones at the benzodiazepine site of GABA(A) receptors.
Lund University
Applications of parallel synthetic lead hopping and pharmacophore-based virtual screening in the discovery of efficient glycine receptor potentiators.
Amgen
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
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.
Yogi Vemana University
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.
University of Leipzig
The amylase inhibitor montbretin A reveals a new glycosidase inhibition motif.
University of British Columbia
Structure-guided design of a high affinity inhibitor to human CtBP.
University of Massachusetts Medical School
Structural Requirements for Eszopiclone and Zolpidem Binding to the gamma-Aminobutyric Acid Type-A (GABAA) Receptor Are Different.
University of Wisconsin At Madison