PMID

Data

Article Title

Organization

Ion channels as therapeutic targets: a drug discovery perspective.

Pfizer

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

Astrazeneca

Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators.

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.

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 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

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

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

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

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

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

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

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

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 Characterization of a Novel?-Aminobutyric Acid Type A (GABA

University of Wisconsin-Milwaukee