ArticleThe Journal of general physiology2014
A nonequilibrium binary elements-based kinetic model for benzodiazepine regulation of GABAA receptors.
Article in The Journal of general physiology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 38 citations in OpenAlex.
- Activation of the human β3 GABABiochemical pharmacology · 2026Article
- Null method to estimate the maximal PA at subsaturating concentrations of agonist.The Journal of general physiology · 2025Article
- Mechanism of acid-sensing ion channel modulation by Hi1a.The Journal of general physiology · 2024Article
- Proline substitutions in the ASIC1 β11-12 linker slow desensitization.Biophysical journal · 2024Article
- Potentiation of the GABABiophysical journal · 2024Article
- State-dependent energetics of GABABiophysical journal · 2024Article
- GABABiophysical journal · 2024Article
- Zinc activation of OTOP proton channels identifies structural elements of the gating apparatus.eLife · 2023Article
- Charge-voltage curves of Shaker potassium channel are not hysteretic at steady state.The Journal of general physiology · 2023Article
- Benzodiazepine Modulation of GABABiomolecules · 2022Review
- A critical residue in the αeLife · 2021Article
- Article
- β11-12 linker isomerization governs acid-sensing ion channel desensitization and recovery.eLife · 2020Article
- GABAFrontiers in cellular neuroscience · 2020Article
- Looking for Novelty in an "Old" Receptor: Recent Advances Toward Our Understanding of GABAFrontiers in neuroscience · 2020Review
- Batrachotoxin acts as a stent to hold open homotetrameric prokaryotic voltage-gated sodium channels.The Journal of general physiology · 2019Article
- Bipolar switching by HCN voltage sensor underlies hyperpolarization activation.Proceedings of the National Academy of Sciences of the United States of America · 2019Article
- Applying the Monod-Wyman-Changeux Allosteric Activation Model to Pseudo-Steady-State Responses from GABAMolecular pharmacology · 2019Review
- Minimal molecular determinants of isoform-specific differences in efficacy in the HCN channel family.The Journal of general physiology · 2018Article
- GABA Type A Receptor Activation in the Allosteric Coagonist Model Framework: Relationship between ECMolecular pharmacology · 2018Article
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Ion channels, like many other proteins, are composed of multiple structural domains. A stimulus that impinges on one domain, such as binding of a ligand to its recognition site, can influence the activity of another domain, such as a transmembrane channel gate, through interdomain interactions. Kinetic schemes that describe the function of interacting domains typically incorporate a minimal number of states and transitions, and do not explicitly model interactions between domains. Here, we develop a kinetic model of the GABAA receptor, a ligand-gated ion channel modulated by numerous compounds including benzodiazepines, a class of drugs used clinically as sedatives and anxiolytics. Our model explicitly treats both the kinetics of distinct functional domains within the receptor and the interactions between these domains. The model describes not only how benzodiazepines that potentiate GABAA receptor activity, such as diazepam, affect peak current dose-response relationships in the presence of desensitization, but also their effect on the detailed kinetics of current activation, desensitization, and deactivation in response to various stimulation protocols. Finally, our model explains positive modulation by benzodiazepines of receptor currents elicited by either full or partial agonists, and can resolve conflicting observations arguing for benzodiazepine modulation of agonist binding versus channel gating.
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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.