PMID

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Article Title

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Synthesis and pharmacological evaluation of pyrazolo[1,5-a]pyrimidin-7(4H)-one derivatives as potential GABA

University of Florence

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

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

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

University of California

Refinement of the benzodiazepine receptor site topology by structure-activity relationships of new N-(heteroarylmethyl)indol-3-ylglyoxylamides.

University of Pisa

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

Synthesis and in vitro activity of 3 beta-substituted-3 alpha-hydroxypregnan-20-ones: allosteric modulators of the GABAA receptor.

Cocensys

Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor.

Heidelberg

Novel Cyclic Phosphinic Acids as GABA_C ρ Receptor Antagonists: Design, Synthesis, and Pharmacology

TBA

Developing dual functional allosteric modulators of GABA(A) receptors.

Astrazeneca Pharmaceuticals

The GABA(A) receptor as a target for photochromic molecules.

University of Massachusetts

 

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

TBA

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

Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands.

Università

Novel 3-iodo-8-ethoxypyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide as promising lead for design of alpha5-inverse agonist useful tools for therapy of mnemonic damage.

Università

4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.

Lund University

Clerodane Diterpenes from

University of Basel

Rationalizing the binding and α subtype selectivity of synthesized imidazodiazepines and benzodiazepines at GABAA receptors by using molecular docking studies.

University of Wisconsin-Milwaukee

High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives.

Università

Structure-Activity Studies of 3,9-Diazaspiro[5.5]undecane-Based γ-Aminobutyric Acid Type A Receptor Antagonists with Immunomodulatory Effect.

University of Copenhagen

Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors.

University of Sydney

Synthesis and Biological Evaluation of Pyrroloindolines as Positive Allosteric Modulators of the α1β2γ2 GABA

California Institute of Technology

Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands.

University of Firenze

Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents.

Università

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

University of Graz

Novel N-(arylalkyl)indol-3-ylglyoxylylamides targeted as ligands of the benzodiazepine receptor: synthesis, biological evaluation, and molecular modeling analysis of the structure-activity relationships.

Università

Discovery of 2-(Imidazo[1,2- b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-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

Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-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.

University of Louvain

GABA allosteric modulators: An overview of recent developments in non-benzodiazepine modulators.

The University of Sydney

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 α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.

Northwest University

Design, Synthesis, and Pharmacological Evaluation of Novel β2/3 Subunit-Selective γ-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 γ-aminobutyric acid type A receptors by piperine derivatives.

University of Vienna

Exploring the orthosteric binding site of the γ-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

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

Homology modeling and atomic level binding study of GABA(A) receptor with novel enaminone amides.

Wuhan Institute of Technology

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

Agonists of the γ-aminobutyric acid type B (GABA

University of Mississippi

A new class of pyrazolo[5,1-c][1,2,4]triazines as γ-aminobutyric type A (GABA

Universita Degli Studi Di Firenze

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 pharmacological evaluation of neurosteroid photoaffinity ligands.

University of Illinois At Chicago

Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)

Sage Therapeutics

Pyrido[2,3-D]Imidazole Derivatives and Their Use As Inhibitors of ITK for the Treatment of Skin Disease

Pfizer

THYROID HORMONE RECEPTOR BETA AGONIST COMPOUNDS

Terns Pharmaceuticals

N2,N4-diphenylpyrimidine-2,4-diamine derivative, method for preparing same, and pharmaceutical composition containing same as active ingredient for prevention or treatment of cancer

Korea Research Institute of Chemical Technology

Benzothiazoles having histamine H3 receptor activity

High Point Pharmaceuticals