ArticleThe Journal of neuroscience : the official journal of the Society for Neuroscience1998
Defining affinity with the GABAA receptor.
Article in The Journal of neuroscience : the official journal of the Society for Neuroscience, 1998. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 74 papers.
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Who cites it
74 citing papers in PubMed.
- Molecular assemblies and pharmacology of cerebellar GABAProceedings of the National Academy of Sciences of the United States of America · 2026Article
- β-Alanine Is an Unexploited Neurotransmitter in the Pathogenesis and Treatment of Alzheimer's Disease.NeuroSci · 2026Review
- Null method to estimate the maximal PA at subsaturating concentrations of agonist.The Journal of general physiology · 2025Article
- The impact of diffusion on receptor binding during synaptic transmission.Biophysical journal · 2024Article
- State-dependent energetics of GABABiophysical journal · 2024Article
- Dynamics of receptor activation by agonists.Biophysical journal · 2024Review
- Changes in Memory, Sedation, and Receptor Kinetics Imparted by the β2-N265M and β3-N265M GABAInternational journal of molecular sciences · 2023Article
- Coupling structure with function in acid-sensing ion channels: challenges in pursuit of proton sensors.The Journal of physiology · 2021Review
- Enhancement of Muscimol Binding and Gating by Allosteric Modulators of the GABAMolecular pharmacology · 2020Article
- GABAFrontiers in cellular neuroscience · 2020Article
- Homotaurine Treatment Enhances CD4ImmunoHorizons · 2019Article
- Amino acid substitutions in the human homomeric βThe Journal of biological chemistry · 2019Article
- Analysis of GABAMolecular pharmacology · 2019Article
- Homotaurine, a safe blood-brain barrier permeable GABAScientific reports · 2018Article
- Deactivation kinetics of acid-sensing ion channel 1a are strongly pH-sensitive.Proceedings of the National Academy of Sciences of the United States of America · 2017Article
- Enhanced desensitization followed by unusual resensitization in GABAA receptors in phospholipase C-related catalytically inactive protein-1/2 double-knockout mice.Pflugers Archiv : European journal of physiology · 2015Article
- Stargazin promotes closure of the AMPA receptor ligand-binding domain.The Journal of general physiology · 2014Article
- Enhancement of α5-containing γ-aminobutyric acid type A receptors by the nonimmobilizer 1,2-dichlorohexafluorocyclobutane (F6) is abolished by the β3(N265M) mutation.Anesthesia and analgesia · 2014Article
- Synaptic GABAA receptor clustering without the γ2 subunit.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2014Article
- Article
14 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
4 authors.
Funding
Abstract
At nicotinic and glutamatergic synapses, the duration of the postsynaptic response depends on the affinity of the receptor for transmitter (Colquhoun et al., 1977;Pan et al., 1993). Affinity is often thought to be determined by the ligand unbinding rate, whereas the binding rate is assumed to be diffusion-limited. In this view, the receptor selects for those ligands that form a stable complex on binding, but binding is uniformly fast and does not itself affect selectivity. We tested these assumptions for the GABAA receptor by dissecting the contributions of microscopic binding and unbinding kinetics for agonists of equal efficacy but of widely differing affinities. Agonist pulses applied to outside-out patches of cultured rat hippocampal neurons revealed that agonist unbinding rates could not account for affinity if diffusion-limited binding was assumed. However, direct measurement of the instantaneous competition between agonists and a competitive antagonist revealed that binding rates were orders of magnitude slower than expected for free diffusion, being more steeply correlated with affinity than were the unbinding rates. The deviation from diffusion-limited binding indicates that a ligand-specific energy barrier between the unbound and bound states determines GABAA receptor selectivity. This barrier and our kinetic observations can be quantitatively modeled by requiring the participation of movable elements within a flexible GABA binding site.
Indexed as
Identifiers
9786967PMC6793556What 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.