ReviewBritish journal of pharmacology2012
A novel GABA(A) receptor pharmacology: drugs interacting with the α(+) β(-) interface.
Review in British journal of pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 46 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
46 citing papers in PubMed.
- GABAJournal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2026Article
- Synaptic correlates of benzodiazepine tolerance.Molecular psychiatry · 2026Review
- Anticonvulsant Potential of the Essential Oil ofACS omega · 2026Article
- Succinic acid enhances sedative activity of diazepam through GABAergic receptor modulation: Evidence from behavioral approach and computational insights.Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- GABADrug design, development and therapy · 2026Review
- Anxiolytic-Like Effects of Citronellal and Phytol, Possibly Through the GABAergic Interaction Pathway: In Vivo with Molecular Docking Studies.Molecular neurobiology · 2025Article
- Antiseizure Medications: Advancements, Challenges, and Prospects in Drug Development.Current neuropharmacology · 2025Review
- A comprehensive In-silico analysis of the known and novel synthesized 5-substituted barbituric acid derivatives acting as CNS depressants.In silico pharmacology · 2025Article
- Evaluation of the sedative-motor effects of novel GABAkine imidazodiazepines using quantitative observation techniques in rhesus monkeys.Journal of psychopharmacology (Oxford, England) · 2024Article
- 3,8-Disubstituted Pyrazolo[1,5-a]quinazoline as GABAInternational journal of molecular sciences · 2024Article
- Modulators of GABANeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2024Review
- Pathogenic variants of human GABRA1 gene associated with epilepsy: A computational approach.Heliyon · 2023Article
- GABAInternational journal of molecular sciences · 2022Article
- Glutamate and GABASignal transduction and targeted therapy · 2022Article
- Dogs as a Natural Animal Model of Epilepsy.Frontiers in veterinary science · 2022Review
- Structural determinants and regulation of spontaneous activity in GABANature communications · 2021Article
- A Targeted Bioinformatics Assessment of Adrenocortical Carcinoma Reveals Prognostic Implications of GABA System Gene Expression.International journal of molecular sciences · 2020Article
- Heterogeneous expression of GABA receptor-like subunits LCCH3 and GRD reveals functional diversity of GABA receptors in the honeybee Apis mellifera.British journal of pharmacology · 2020Article
- Allosteric GABAMolecules (Basel, Switzerland) · 2020Review
- Structure-Guided Computational Methods Predict Multiple Distinct Binding Modes for Pyrazoloquinolinones in GABAFrontiers in neuroscience · 2020Article
Corrections and comments
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Authors and funding
5 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
GABA(A) receptors are ligand-gated chloride channels composed of five subunits that can belong to different subunit classes. The existence of 19 different subunits gives rise to a multiplicity of GABA(A) receptor subtypes with distinct subunit composition; regional, cellular and subcellular distribution; and pharmacology. Most of these receptors are composed of two α, two β and one γ2 subunits. GABA(A) receptors are the site of action of a variety of pharmacologically and clinically important drugs, such as benzodiazepines, barbiturates, neuroactive steroids, anaesthetics and convulsants. Whereas GABA acts at the two extracellular β(+) α(-) interfaces of GABA(A) receptors, the allosteric modulatory benzodiazepines interact with the extracellular α(+) γ2(-) interface. In contrast, barbiturates, neuroactive steroids and anaesthetics seem to interact with solvent accessible pockets in the transmembrane domain. Several benzodiazepine site ligands have been identified that selectively interact with GABA(A) receptor subtypes containing α2βγ2, α3βγ2 or α5βγ2 subunits. This indicates that the different α subunit types present in these receptors convey sufficient structural differences to the benzodiazepine binding site to allow specific interaction with certain benzodiazepine site ligands. Recently, a novel drug binding site was identified at the α(+) β(-) interface. This binding site is homologous to the benzodiazepine binding site at the α(+) γ2(-) interface and is thus also strongly influenced by the type of α subunit present in the receptor. Drugs interacting with this binding site cannot directly activate but only allosterically modulate GABA(A) receptors. The possible importance of such drugs addressing a spectrum of receptor subtypes completely different from that of benzodiazepines is discussed.
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