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 |
| 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 |
| 18537233 |
108 |
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit. |
Moltech |
| 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 |
| 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 |
| | 7 |
A conformational study of ligands for omega modulatory sites of GABAa receptors by NOESY NMR spectroscopy and distance geometry |
TBA |
| 16610803 |
40 |
A pyridazine series of alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety. |
Merck Sharp & Dohme Research Laboratories |
| 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 |
| 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 |
| 16162003 |
78 |
A new pyridazine series of GABAA alpha5 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 |
| 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 |
| 12408715 |
97 |
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 |
| 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 |
| 11412984 |
66 |
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors. |
The Royal Danish School Of Pharmacy |
| 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 |
| 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 |
| 21406034 |
34 |
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 |
| 26214255 |
11 |
The amylase inhibitor montbretin A reveals a new glycosidase inhibition motif. |
University Of British Columbia |
| 25636004 |
12 |
Structure-guided design of a high affinity inhibitor to human CtBP. |
University Of Massachusetts Medical School |
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