ArticleThe Journal of neuroscience : the official journal of the Society for Neuroscience2002
Desensitization mechanism of GABA receptors revealed by single oocyte binding and receptor function.
Article in The Journal of neuroscience : the official journal of the Society for Neuroscience, 2002. 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 52 papers.
What it found
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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.
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
52 citing papers in PubMed, 71 citations in OpenAlex.
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- Subtype-Specific Ligand Binding and Activation Gating in Homomeric and Heteromeric P2X Receptors.Biomolecules · 2024Article
- Alfaxalone does not have long-term effects on goldfish pyramidal neuron action potential properties or GABAFEBS open bio · 2024Article
- Neurosteroid Binding and Actions on GABAJuntendo Iji zasshi = Juntendo medical journal · 2024Review
- Functional properties of GABAFrontiers in ophthalmology · 2023Article
- Physiological Role of ATPase for GABAInternational journal of molecular sciences · 2022Article
- The Influence of AA29504 on GABANeurochemical research · 2022Article
- The Sulfated Steroids Pregnenolone Sulfate and Dehydroepiandrosterone Sulfate Inhibit theMolecular pharmacology · 2022Article
- Electrophysiology of ionotropic GABA receptors.Cellular and molecular life sciences : CMLS · 2021Review
- Enhancement of Muscimol Binding and Gating by Allosteric Modulators of the GABAMolecular pharmacology · 2020Article
- Site-specific effects of neurosteroids on GABAeLife · 2020Article
- Simple ammonium salts acting on sigma-1 receptors yield potential treatments for cancer and depression.Scientific reports · 2020Article
- Image-Based Marker-Free Screening of GABASLAS discovery : advancing life sciences R & D · 2020Article
- Molecular and Regulatory Mechanisms of Desensitization and Resensitization of GABAInternational journal of molecular sciences · 2020Review
- Mechanism and effects of pulsatile GABA secretion from cytosolic pools in the human beta cell.Nature metabolism · 2019Article
- Extrasynaptic δ-GABAJournal of neurochemistry · 2019Article
- GABANature · 2019Article
Corrections and comments
- Erratum issuedChang YongChang [corrected to Chang Yongchang]
Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
Prolonged exposure of most fast neurotransmitter-operated ion channels to agonist drives the receptors into a nonfunctional, or desensitized, state. Despite extensive investigation, desensitization remains a thoroughly characterized, yet poorly understood, process. Part of the difficulty in elucidating the mechanism of desensitization has been an inability to resolve the kinetics of both agonist binding and functional desensitization in the same set of operable receptors. To overcome this limitation, we applied single oocyte 3H-ligand binding and two-electrode voltage clamp to oocytes expressing recombinant alpha1beta2gamma2 GABA receptors. Using this approach, we report several observations fundamental to the mechanism of desensitization. First, we confirm that desensitization reversibly shifts GABA receptors into a high-affinity state. For [3H]GABA binding, the half-maximal binding of the desensitized state was approximately 0.040 microm. Second, we show that, upon agonist removal, this high-affinity state disappears with a time constant of 127 +/- 12 sec (n = 4), similar to the time constant for functional recovery from desensitization of 124 +/- 26 sec (n = 5). [3H]GABA, however, dissociates fourfold faster (tau = 30 +/- 2 sec; n = 3) than functional recovery, indicating that desensitized receptors need not be bound by GABA. These data provide direct evidence for a cyclical model of receptor desensitization.
Indexed as
Identifiers
12223551PMC6758118W2150786660What 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.