PMID

Data

Article Title

Organization

Ion channels as therapeutic targets: a drug discovery perspective.

Pfizer

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

Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.

Moltech

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

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

 

A conformational study of ligands for omega modulatory sites of GABAa receptors by NOESY NMR spectroscopy and distance geometry

TBA

Multiparameter Optimization of Naphthyridine Derivatives as Selective ?5-GABA

Gedeon Richter

A pyridazine series of alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.

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.

TBA

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

A new pyridazine series of GABAA alpha5 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

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

Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.

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.

Neurogen

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

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

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

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

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

An overview of benzo[b]thiophene-based medicinal chemistry.

Jain University

The preparation, in vitro screening and molecular docking of symmetrical bisquaternary cholinesterase inhibitors containing a but-(2E)-en-1,4-diyl connecting linkage.

University of Defence

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

Design and synthesis of a tetrahydroisoquinoline-based hydroxamate derivative (ZYJ-34v), an oral active histone deacetylase inhibitor with potent antitumor activity.

Shandong University

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