The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 23121096 |
86 |
Ion channels as therapeutic targets: a drug discovery perspective. |
Pfizer |
| 21498079 |
45 |
Development and SAR of functionally selective allosteric modulators of GABAA receptors. |
Astrazeneca |
| 22734650 |
6 |
Allyl m-trifluoromethyldiazirine mephobarbital: an unusually potent enantioselective and photoreactive barbiturate general anesthetic. |
Massachusetts General Hospital |
| 19726184 |
62 |
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 |
| 17470817 |
12 |
Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators. |
University of California |
| 17375905 |
20 |
4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships. |
University of Copenhagen |
| 16392789 |
66 |
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 |
| 11606122 |
7 |
Alpha-amino acid phenolic ester derivatives: novel water-soluble general anesthetic agents which allosterically modulate GABA(A) receptors. |
Organon Research and Development Group |
| 10633039 |
718 |
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach. |
University of Wisconsin-Milwaukee |
| 15125950 |
56 |
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors. |
Merck |
| 21163663 |
15 |
Triazoloquinazolinediones as novel high affinity ligands for the benzodiazepine site of GABA(A) receptors. |
Lund University |
| 20980155 |
24 |
Developing dual functional allosteric modulators of GABA(A) receptors. |
Astrazeneca Pharmaceuticals |
| 20646926 |
13 |
The GABA(A) receptor as a target for photochromic molecules. |
University of Massachusetts |
| 20888240 |
254 |
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 |
| 19762240 |
62 |
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 |
| 19740657 |
42 |
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 |
| 17544280 |
50 |
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 |
| 16621541 |
38 |
2,3,7-Trisubstituted pyrazolo[1,5-d][1,2,4]triazines: functionally selective GABAA alpha3-subtype agonists. |
Merck Sharp and Dohme Research Laboratories |
| 16610803 |
40 |
A pyridazine series of alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety. |
Merck Sharp & Dohme Research Laboratories |
| 16480274 |
11 |
Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology. |
The Danish University of Pharmaceutical Sciences |
| 16480260 |
26 |
Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety. |
TBA |
| 16406613 |
40 |
Imidazo[1,2-a]pyrimidines as functionally selective GABA(A) ligands. |
Merck Sharp and Dohme Research Laboratories |
| 16386901 |
6 |
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 |
| 16386900 |
50 |
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 |
| 16384707 |
27 |
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 |
| 16279764 |
29 |
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 |
| 16162003 |
78 |
A new pyridazine series of GABAA alpha5 ligands. |
Merck Sharp & Dohme Research Laboratories |
| 16153832 |
2 |
Pyrazolopyridinones as functionally selective GABAA ligands. |
Merck Sharp & Dohme Research Laboratories |
| 15743180 |
404 |
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 |
| 15537339 |
18 |
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties. |
Merck Sharp & Dohme Research Laboratories |
| 15214791 |
147 |
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 |
| 15177449 |
31 |
2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor. |
Merck Sharp & Dohme Research Laboratories |
| 15084116 |
48 |
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers. |
Merck Sharp and Dohme Research Laboratories |
| 15027873 |
247 |
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 |
| 15026049 |
42 |
Tricyclic pyridones as functionally selective human GABAA alpha 2/3 receptor-ion channel ligands. |
The Neuroscience Research Centre |
| 15006383 |
12 |
Determination of the stable conformation of GABA(A)-benzodiazepine receptor bivalent ligands by low temperature NMR and X-ray analysis. |
University of Wisconsin-Milwaukee |
| 14667209 |
32 |
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 |
| 12747794 |
124 |
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition. |
Merck Sharp & Dohme Research Laboratories |
| 11960500 |
109 |
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 |
| 11881985 |
48 |
6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists. |
Merck Sharp & Dohme Research Laboratories |
| 11677140 |
4 |
Fipronil-based photoaffinity probe for Drosophila and human beta 3 GABA receptors. |
University of California |
| 11412984 |
66 |
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors. |
The Royal Danish School of Pharmacy |
| 10890169 |
48 |
N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit. |
Merck Sharp & Dohme Research Laboratories |
| 31738537 |
95 |
Subtype Selective ?-Aminobutyric Acid Type A Receptor (GABA |
University of Sussex |
| 30964988 |
26 |
Design and Identification of a Novel, Functionally Subtype Selective GABA |
Pfizer |
| 9767648 |
275 |
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 |
| 30928713 |
14 |
GABA allosteric modulators: An overview of recent developments in non-benzodiazepine modulators. |
The University of Sydney |
| 9651158 |
158 |
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 |
| 30289721 |
26 |
Design, Synthesis, and Pharmacological Evaluation of Novel ?2/3 Subunit-Selective ?-Aminobutyric Acid Type A (GABA |
University of Vienna |
| 24905252 |
17 |
Efficient modulation of ?-aminobutyric acid type A receptors by piperine derivatives. |
University of Vienna |
| 24462176 |
3 |
Identification of dihydrostilbenes in Pholidota chinensis as a new scaffold for GABAA receptor modulators. |
University of Basel |
| 21751815 |
4 |
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£ |
| 28606760 |
57 |
Progress in the discovery of small molecule modulators of the Cys-loop superfamily receptors. |
Amgen |
| 29146472 |
71 |
Discovery of the first low-shift positive allosteric modulators for the muscarinic M1 receptor. |
Roche Pharma Research and Early Development |
| 28505538 |
9 |
Synthesis and pharmacological evaluation of neurosteroid photoaffinity ligands. |
University of Illinois At Chicago |
| 27933953 |
23 |
Synthesis and Characterization of a Novel?-Aminobutyric Acid Type A (GABA |
University of Wisconsin-Milwaukee |
| 28753313 |
45 |
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 |
| 18790643 |
42 |
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 |
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