ArticleAnesthesiology2012
An allosteric coagonist model for propofol effects on α1β2γ2L γ-aminobutyric acid type A receptors.
Article in Anesthesiology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 53 papers.
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Who cites it
53 citing papers in PubMed, 65 citations in OpenAlex.
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- Age-dependent electroencephalogram alterations under remimazolam anesthesia.Korean journal of anesthesiology · 2026Observational
- Propofol for depression: mechanisms and therapeutic potential.Frontiers in physiology · 2026Review
- Comparison of Cognitive Deterioration Between Propofol and Remimazolam Anesthesia in ApoE4 Knock-In Mouse Model.International journal of molecular sciences · 2025Article
- Null method to estimate the maximal PA at subsaturating concentrations of agonist.The Journal of general physiology · 2025Article
- State-dependent energetics of GABABiophysical journal · 2024Article
- Potentiation of the GABABiophysical journal · 2024Article
- Mutational Analysis of Anesthetic Binding Sites and Their Effects on GABABiomolecules · 2023Article
- Safety and effectiveness of the combination of remimazolam tosilate and propofol in gastroscopy: a multicenter, randomized controlled, single-blind clinical trial.Frontiers in pharmacology · 2023Article
- Photomotor Responses in Zebrafish and Electrophysiology Reveal Varying Interactions of Anesthetics Targeting Distinct Sites on γ-Aminobutyric Acid Type A Receptors.Anesthesiology · 2022Article
- Efficacy and safety of different doses of remimazolam tosylate for colonoscopy: single-center, prospective, randomized, double-blind, parallel trial.Annals of translational medicine · 2022Article
- Isoflurane inhibition of endocytosis is an anesthetic mechanism of action.Current biology : CB · 2022Article
- Activation of the Rat α1β2ε GABABiomolecules · 2022Article
- Perspective on the Relationship between GABAA Receptor Activity and the Apparent Potency of an Inhibitor.Current neuropharmacology · 2022Article
- Selective actions of benzodiazepines at the transmembrane anaesthetic binding sites of the GABABritish journal of pharmacology · 2021Article
- Magnetic Resonance Imaging (MRI) and Spectroscopy in Succinic Semialdehyde Dehydrogenase Deficiency.Journal of child neurology · 2021Article
- Electrophysiology of ionotropic GABA receptors.Cellular and molecular life sciences : CMLS · 2021Review
- Direct Structural Insights into GABATrends in biochemical sciences · 2021Review
- Modulation of α1β3γ2 GABAProceedings of the National Academy of Sciences of the United States of America · 2021Article
- Anesthesia-Induced Oxidative Stress: Are There Differences between Intravenous and Inhaled Anesthetics?Oxidative medicine and cellular longevity · 2021Review
Corrections and comments
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Authors and funding
4 authors at 3 institutions in 2 countries.
Funding
Abstract
backgroundPropofol produces its major actions via γ-aminobutyric acid type A (GABA(A)) receptors. At low concentrations, propofol enhances agonist-stimulated GABA(A) receptor activity, and high propofol concentrations directly activate receptors. Etomidate produces similar effects, and there is convincing evidence that a single class of etomidate sites mediate both agonist modulation and direct GABA(A) receptor activation. It is unknown if the propofol binding site(s) on GABA(A) receptors that modulate agonist-induced activity also mediate direct activation.
methodsGABA(A) α1β2γ2L receptors were heterologously expressed in Xenopus oocytes and activity was quantified using voltage clamp electrophysiology. We tested whether propofol and etomidate display the same linkage between agonist modulation and direct activation of GABA(A) receptors by identifying equiefficacious drug solutions for direct activation. We then determined whether these drug solutions produce equal modulation of GABA-induced receptor activity. We also measured propofol-dependent direct activation and modulation of low GABA responses. Allosteric coagonist models similar to that established for etomidate, but with variable numbers of propofol sites, were fitted to combined data.
resultsSolutions of 19 μM propofol and 10 μM etomidate were found to equally activate GABA(A) receptors. These two drug solutions also produced indistinguishable modulation of GABA-induced receptor activity. Combined electrophysiological data behaved in a manner consistent with allosteric coagonist models with more than one propofol site. The best fit was observed when the model assumed three equivalent propofol sites.
conclusionsOur results support the hypothesis that propofol, like etomidate, acts at GABA(A) receptor sites mediating both GABA modulation and direct activation.
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