ArticleThe Journal of physiology2011
Transmembrane AMPA receptor regulatory protein regulation of competitive antagonism: a problem of interpretation.
Article in The Journal of physiology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 27 citations in OpenAlex.
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- Identification of a Subpopulation of Astrocyte Progenitor Cells in the Neonatal Subventricular Zone: Evidence that Migration is Regulated by Glutamate Signaling.Neurochemical research · 2025Article
- Activity Dependent Inhibition of AMPA Receptors by ZnThe Journal of neuroscience : the official journal of the Society for Neuroscience · 2020Article
- Mechanism of modulation of AMPA receptors by TARP-γ8.The Journal of general physiology · 2020Article
- Chronic Ethanol Exposure and Withdrawal Impair Synaptic GABAAlcoholism, clinical and experimental research · 2019Article
- Polyamine-mediated channel block of ionotropic glutamate receptors and its regulation by auxiliary proteins.The Journal of biological chemistry · 2018Review
- Article
- Enhanced incentive motivation in obesity-prone rats is mediated by NAc core CP-AMPARs.Neuropharmacology · 2018Article
- Stargazin Modulation of AMPA Receptors.Cell reports · 2016Article
- Train stimulation of parallel fibre to Purkinje cell inputs reveals two populations of synaptic responses with different receptor signatures.The Journal of physiology · 2016Article
- Superactivation of AMPA receptors by auxiliary proteins.Nature communications · 2016Article
- Stargazin promotes closure of the AMPA receptor ligand-binding domain.The Journal of general physiology · 2014Article
- RNA based antagonist of NMDA receptors.ACS chemical neuroscience · 2014Article
- Auxiliary proteins promote modal gating of AMPA- and kainate-type glutamate receptors.The European journal of neuroscience · 2014Article
- CrossTalk proposal: TARPs modulate AMPA receptor gating transitions.The Journal of physiology · 2013Article
- RIM3γ and RIM4γ are key regulators of neuronal arborization.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2013Article
- Stargazing from a new vantage--TARP modulation of AMPA receptor pharmacology.The Journal of physiology · 2011Article
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2 authors at 1 institution in 1 country.
Funding
Abstract
Synaptic AMPA receptors are greatly influenced by a family of transmembrane AMPA receptor regulatory proteins (TARPs) which control trafficking, channel gating and pharmacology. The prototypical TARP, stargazin (or γ2), shifts the blocking ability of several AMPAR-selective compounds including the commonly used quinoxalinedione antagonists, CNQX and NBQX. Stargazin's effect on CNQX is particularly intriguing as it not only apparently lowers the potency of block, as with NBQX, but also renders it a partial agonist. Given this, agonist behaviour by CNQX has been speculated to account for its weaker blocking effect on AMPAR-TARP complexes. Here we show that this is not the case. The apparent effect of stargazin on CNQX antagonism can be almost entirely explained by an increase in the apparent affinity for l-glutamate (l-Glu), a full agonist and neurotransmitter at AMPAR synapses. Partial agonism at best plays a minor role but not through channel gating per se but rather because CNQX elicits AMPAR desensitization. Our study reveals that CNQX is best thought of as a non-competitive antagonist at glutamatergic synapses due to the predominance of non-equilibrium conditions. Consequently, CNQX primarily reports the proportion of AMPARs available for activation but may also impose additional block by receptor desensitization.
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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.