A Benzodiazepine Ligand with Improved GABAA Receptor α5-Subunit Selectivity Driven by Interactions with Loop C

Neurobiology and Therapeutic Potential of α5-GABA Type A Receptors

(2019) Tija C. Jacob   Frontiers in Molecular Neuroscience

Engineered flumazenil recognition site provides mechanistic insight governing benzodiazepine modulation in GABAA receptors

(2018) David C. B. Siebert et al.   ACS Chemical Biology

Different Benzodiazepines Bind with Distinct Binding Modes to GABAA Receptors

(2018) Alshaimaa A. Elgarf et al.   ACS Chemical Biology

A Novel Orally Available Asthma Drug Candidate That Reduces Smooth Muscle Constriction and Inflammation by Targeting GABAA Receptors in the Lung

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Cryo-EM structure of the human α5β3 GABAA receptor

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Structure of a human synaptic GABAA receptor

(2018) Shaotong Zhu et al.   NATURE

Cryo-EM structure of the benzodiazepine-sensitive α1β1γ2S tri-heteromeric GABAA receptor in complex with GABA

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GABAA receptor signalling mechanisms revealed by structural pharmacology

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International Union of Basic and Clinical Pharmacology. CVI: GABAA Receptor Subtype- and Function-selective Ligands: Key Issues in Translation to Humans

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Alleviation of Multiple Asthmatic Pathologic Features with Orally Available and Subtype Selective GABAA Receptor Modulators

(2017) Gloria S. Forkuo et al.   MOLECULAR PHARMACEUTICS

Binding site opening by loop C shift and chloride ion-pore interaction in the GABAA receptor model

(2017) M. A. Michałowski et al.   PHYSICAL CHEMISTRY CHEMICAL PHYSICS

Molecular tools for GABAA receptors: High affinity ligands for β1-containing subtypes

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Targeting the γ-Aminobutyric Acid A Receptor α4 Subunit in Airway Smooth Muscle to Alleviate Bronchoconstriction

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Ester to amide substitution improves selectivity, efficacy and kinetic behavior of a benzodiazepine positive modulator of GABA A receptors containing the α5 subunit

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GABAergic signalling in the immune system

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Selective targeting of the α5-subunit of GABAA receptors relaxes airway smooth muscle and inhibits cellular calcium handling

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Dopamine Directly Modulates GABAA Receptors

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GABAergic system in the endocrine pancreas: a new target for diabetes treatment

(2015) Qinghua Wang et al.   Diabetes Metabolic Syndrome and Obesity-Targets and Therapy

Accelerated Discovery of Novel Benzodiazepine Ligands by Experiment-Guided Virtual Screening

(2014) Simon J. Middendorp et al.   ACS Chemical Biology

The Role of α5 GABAA Receptor Agonists in the Treatment of Cognitive Deficits in Schizophrenia

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α5-GABAA receptors negatively regulate MYC-amplified medulloblastoma growth

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GABAAReceptor Subtypes: Therapeutic Potential in Down Syndrome, Affective Disorders, Schizophrenia, and Autism

(2013) Uwe Rudolph et al.   Annual Review of Pharmacology and Toxicology

Enhancing the function of alpha5-subunit-containing GABAA receptors promotes action potential firing of neocortical neurons during up-states

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A Closer Look at the High Affinity Benzodiazepine Binding Site on GABAA Receptors

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Diazepam-bound GABAA receptor models identify new benzodiazepine binding-site ligands

(2012) Lars Richter et al.   Nature Chemical Biology

Extrasynaptic GABAA Receptors: Their Function in the CNS and Implications for Disease

(2012) Stephen G. Brickley et al.   NEURON

Influence of GABAA Receptor α Subunit Isoforms on the Benzodiazepine Binding Site

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Histamine-gated ion channels in mammals?

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Flavonoid modulation of GABAA receptors

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Different Residues in the GABAA Receptor Benzodiazepine Binding Pocket Mediate Benzodiazepine Efficacy and Binding

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The major central endocannabinoid directly acts at GABAA receptors

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Valerenic acid derivatives as novel subunit-selective GABAA receptor ligands -in vitro and in vivo characterization

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Anxiolytic-like effects of 8-acetylene imidazobenzodiazepines in a rhesus monkey conflict procedure

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The rise of a new GABA pharmacology

(2010) Hanns Möhler   NEUROPHARMACOLOGY

Novel positive allosteric modulators of GABAA receptors: Do subtle differences in activity at α1 plus α5 versus α2 plus α3 subunits account for dissimilarities in behavioral effects in rats?

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A two step synthesis of BzR/GABAergic active flavones via a Wacker-related oxidation

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GABAA receptors are expressed and facilitate relaxation in airway smooth muscle

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Histamine Action on Vertebrate GABAAReceptors

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International Union of Pharmacology. LXX. Subtypes of  -Aminobutyric AcidA Receptors: Classification on the Basis of Subunit Composition, Pharmacology, and Function. Update

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