ArticleThe Journal of general physiology2002
Openings of the rat recombinant alpha 1 homomeric glycine receptor as a function of the number of agonist molecules bound.
Article in The Journal of general physiology, 2002. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 papers.
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Who cites it
38 citing papers in PubMed.
- New hyperekplexia mutations provide insight into glycine receptor assembly, trafficking, and activation mechanisms.The Journal of biological chemistry · 2013Trial
- Exploring the Activation Process of the Glycine Receptor.Journal of the American Chemical Society · 2024Article
- Structural basis for cannabinoid-induced potentiation of alpha1-glycine receptors in lipid nanodiscs.Nature communications · 2022Article
- Advances in hyperekplexia and other startle syndromes.Neurological sciences : official journal of the Italian Neurological Society and of the Italian Society of Clinical Neurophysiology · 2021Review
- The role of tonic glycinergic conductance in cerebellar granule cell signalling and the effect of gain-of-function mutation.The Journal of physiology · 2019Article
- A novel nonsense autosomal dominant mutation in the GLRA1 gene causing hyperekplexia.Journal of neural transmission (Vienna, Austria : 1996) · 2018Article
- Defects of the Glycinergic Synapse in Zebrafish.Frontiers in molecular neuroscience · 2016Review
- The impact of human hyperekplexia mutations on glycine receptor structure and function.Molecular brain · 2014Review
- Principles of agonist recognition in Cys-loop receptors.Frontiers in physiology · 2014Review
- Propofol modulation of α1 glycine receptors does not require a structural transition at adjacent subunits that is crucial to agonist-induced activation.ACS chemical neuroscience · 2013Article
- The kinetic properties of the α3 rat glycine receptor make it suitable for mediating fast synaptic inhibition.The Journal of physiology · 2013Article
- An outline of desensitization in pentameric ligand-gated ion channel receptors.Cellular and molecular life sciences : CMLS · 2013Review
- Activation of trimeric P2X2 receptors by fewer than three ATP molecules.Molecular pharmacology · 2012Article
- 4-Chloropropofol enhances chloride currents in human hyperekplexic and artificial mutated glycine receptors.BMC neurology · 2012Article
- The α1K276E startle disease mutation reveals multiple intermediate states in the gating of glycine receptors.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2012Article
- α7-Containing and non-α7-containing nicotinic receptors respond differently to spillover of acetylcholine.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2011Article
- Chloride ions in the pore of glycine and GABA channels shape the time course and voltage dependence of agonist currents.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2011Article
- The long activations of α2 glycine channels can be described by a mechanism with reaction intermediates ("flip").The Journal of general physiology · 2011Article
- Molecular requirements for ethanol differential allosteric modulation of glycine receptors based on selective Gbetagamma modulation.The Journal of biological chemistry · 2010Article
- Magnitude of a conformational change in the glycine receptor beta1-beta2 loop is correlated with agonist efficacy.The Journal of biological chemistry · 2009Article
Corrections and comments
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Authors and funding
4 authors.
Funding
Abstract
The functional properties of rat homomeric alpha 1 glycine receptors were investigated using whole-cell and outside-out recording from human embryonic kidney cells transfected with rat alpha1 subunit cDNA. Whole-cell dose-response curves gave EC(50) estimates between 30 and 120 microM and a Hill slope of approximately 3.3. Single channel recordings were obtained by steady-state application of glycine (0.3, 1, or 10 microM) to outside-out patches. Single channel conductances were mostly 60-90 pS, but smaller conductances of approximately 40 pS were also seen (10% of the events) with a relative frequency that did not depend on agonist concentration. The time constants of the apparent open time distributions did not vary with agonist concentration, but short events were more frequent at low glycine concentrations. There was also evidence of a previously missed short-lived open state that was more common at lower glycine concentrations. The time constants for the different components of the burst length distributions were found to have similar values at different concentrations. Nevertheless, the mean burst length increased with increasing glycine. This was because the relative area of each burst-length component was concentration dependent and short bursts were favored at lower glycine concentrations. Durations of adjacent open and shut times were found to be strongly (negatively) correlated. Additionally, long bursts were made up of longer than average openings separated by short gaps, whereas short bursts usually consisted of single isolated short openings. The most plausible explanation for these findings is that long bursts are generated when a higher proportion of the five potential agonist binding sites on the receptor is occupied by glycine. On the basis of the concentration dependence and the intraburst structure we provide a preliminary kinetic scheme for the activation of the homomeric glycine receptor, in which any number of glycine molecules from one to five can open the channel, although not with equal efficiency.
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