ArticleThe Journal of neuroscience : the official journal of the Society for Neuroscience2003
Individual properties of the two functional agonist sites in GABA(A) receptors.
Article in The Journal of neuroscience : the official journal of the Society for Neuroscience, 2003. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 69 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
69 citing papers in PubMed, 134 citations in OpenAlex.
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- Molecular Mechanisms and Probe-Dependent Effects of Clinically Relevant GABAArchiv der Pharmazie · 2026Article
- AlphaFold-Multimer modelling of linked nAChR subunits challenges concatemer design assumptions.Scientific reports · 2026Article
- Exploring the role of zolpidem in alleviating cognitive and motor impairments in chronic cerebral hypoperfusion: a rat model study with in vivo and in silico insights.Experimental animals · 2026Article
- Proteostasis regulation of GABABiomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2025Review
- Evaluating Remimazolam for Procedural Sedation.Current neuropharmacology · 2025Review
- Probes for the heterogeneity of muscimol binding sites in rat brain.Frontiers in pharmacology · 2024Article
- Structure-function Studies of GABA (A) Receptors and Related computer-aided Studies.Journal of molecular neuroscience : MN · 2023Review
- Mutational Analysis of Anesthetic Binding Sites and Their Effects on GABABiomolecules · 2023Article
- Allosteric modulation of α1β3γ2 GABABiophysical journal · 2023Article
- Shisa7-Dependent Regulation of GABAThe Journal of neuroscience : the official journal of the Society for Neuroscience · 2022Article
- Unravelling the Turn-On Fluorescence Mechanism of a Fluorescein-Based Probe in GABAAngewandte Chemie (Weinheim an der Bergstrasse, Germany) · 2022Article
- Unravelling the Turn-On Fluorescence Mechanism of a Fluorescein-Based Probe in GABAAngewandte Chemie (International ed. in English) · 2022Article
- GABAkines - Advances in the discovery, development, and commercialization of positive allosteric modulators of GABAPharmacology & therapeutics · 2022Review
- Analyzing the mechanisms that facilitate the subtype-specific assembly ofFrontiers in molecular neuroscience · 2022Article
- GABAJournal, genetic engineering & biotechnology · 2021Review
- Electrophysiology of ionotropic GABA receptors.Cellular and molecular life sciences : CMLS · 2021Review
- Article
- Cryo-electron microscopy reveals informative details of GABAAnnals of translational medicine · 2019Article
- Concatenated γ-aminobutyric acid type A receptors revisited: Finding order in chaos.The Journal of general physiology · 2019Article
9 more citing papers are in PubMed but not listed here.
Corrections and comments
- Erratum issued
Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The members of the pentameric ligand-gated receptor channel family are involved in information transfer in synapses and the neuromuscular junction. They often contain several copies of the same subunit isoform. Here, we present a method to functionally dissect the role of individual subunits that occur in multiple copies in these receptors. Opening of the inherent chloride channel in the GABA(A) receptor is achieved through the binding of two agonist molecules; however, it has been difficult to obtain information on the contribution of the two individual binding sites. The sites are both located at beta+/alpha- subunit interfaces, suggesting similar properties. One pair of subunits is flanked by gamma and beta (site 1) and the other by alpha and gamma (site 2), the different environment possibly affecting the binding sites. Here, we used concatenated subunits and two point mutations of amino acid residues, each in alpha and beta subunits, both located in the agonist binding pocket, to investigate the properties of these two sites. The sites were individually mutated, and consequences of these mutations on GABA and muscimol-induced channel opening and its competitive inhibition by bicuculline were studied. A model predicts that opening also occurs for receptors occupied with a single agonist molecule but is promoted approximately 60-fold in those occupied by two agonists and that site 2 has an approximately threefold higher affinity for GABA than site 1, whereas muscimol and bicuculline show some preference for site 1.
Indexed as
Identifiers
14657175PMC6741049W1948082071What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.