PMID

Data

Article Title

Organization

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

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£

Ion channels as therapeutic targets: a drug discovery perspective.

Pfizer

Synthesis, pharmacological studies and molecular modeling of some tetracyclic 1,3-diazepinium chlorides.

University of The West Indies

Development and SAR of functionally selective allosteric modulators of GABAA receptors.

Astrazeneca

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

Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acid(A) receptor ligands: synthesis, pharmacology, and structure-activity relationships.

University of Copenhagen

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

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.

Universit£

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 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.

Universit£

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

Novel Cyclic Phosphinic Acids as GABA_C 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

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

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

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

Clerodane Diterpenes from

University of Basel

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

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

A new chromanone derivative isolated from Hypericum lissophloeus (Hypericaceae) potentiates GABAA receptor currents in a subunit specific fashion.

University of Graz

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

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

Subtype Selective ?-Aminobutyric Acid Type A Receptor (GABA

University of Sussex

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£

Design and Identification of a Novel, Functionally Subtype Selective GABA

Pfizer

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

The discovery and optimization of benzimidazoles as selective Na

Pfizer

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

Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor.

Upjohn Laboratories

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

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£

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

Optimization of novel monobactams with activity against carbapenem-resistant Enterobacteriaceae - Identification of LYS228.

Novartis Institutes For Biomedical Research

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

Structural Requirements for Eszopiclone and Zolpidem Binding to the gamma-Aminobutyric Acid Type-A (GABAA) Receptor Are Different.

University of Wisconsin At Madison

A study of the structure-activity relationship of GABA(A)-benzodiazepine receptor bivalent ligands by conformational analysis with low temperature NMR and X-ray analysis.

University of Wisconsin-Milwaukee