ArticleBiophysical journal1998
Open channel block and alteration of N-methyl-D-aspartic acid receptor gating by an analog of phencyclidine.
Article in Biophysical journal, 1998. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 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.
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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.
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Who cites it
16 citing papers in PubMed, 31 citations in OpenAlex.
- New advances in small molecule drugs targeting NMDA receptors.Acta pharmacologica Sinica · 2026Review
- Structural insights into function of ionotropic glutamate receptors.Biochemistry (Moscow) Supplement. Series A, Membrane and cell biology · 2022Article
- Historical Pathways for Opioid Addiction, Withdrawal with Traditional and Alternative Treatment Options with Ketamine, Cannabinoids, and Noribogaine: A Narrative Review.Health psychology research · 2022Article
- Interplay between Gating and Block of Ligand-Gated Ion Channels.Brain sciences · 2020Review
- Hydroxynorketamine BlocksMolecular pharmacology · 2020Article
- Effects of MgNeuropharmacology · 2018Article
- NMDA receptors: linking physiological output to biophysical operation.Nature reviews. Neuroscience · 2017Review
- Specific sites within the ligand-binding domain and ion channel linkers modulate NMDA receptor gating.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2010Article
- Mechanisms of the inhibition of endplate acetylcholine receptors by antiseptic chlorhexidine (experiments and models).Naunyn-Schmiedeberg's archives of pharmacology · 2009Article
- Modeling study of mecamylamine block of muscle type acetylcholine receptors.European biophysics journal : EBJ · 2008Article
- Subunit-specific mechanisms and proton sensitivity of NMDA receptor channel block.The Journal of physiology · 2007Article
- Amantadine inhibits NMDA receptors by accelerating channel closure during channel block.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2005Article
- Voltage-dependent inhibition of recombinant NMDA receptor-mediated currents by 5-hydroxytryptamine.British journal of pharmacology · 2005Article
- Free intracellular Mg(2+) concentration and inhibition of NMDA responses in cultured rat neurons.The Journal of physiology · 2001Article
- Quantitative analysis of tetrapentylammonium-induced blockade of open N-methyl-D-aspartate channels.Biophysical journal · 2000Article
- The trapping block of NMDA receptor channels in acutely isolated rat hippocampal neurones.The Journal of physiology · 2000Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
We investigated inhibition of the N-methyl-D-aspartic acid (NMDA) receptor-channel complex by N-ethyl-1,4,9, 9alpha-tetrahydro-4alphaR-cis-4alphaH-fluoren-++ +4alpha-amine (NEFA), a structural analog of phencyclidine (PCP). Using the whole-cell recording technique, we demonstrated that NEFA inhibits NMDA responses with an IC50 of 0.51 microM at -66 mV. We determined that NEFA binds to the open channel, and subsequently the channel can close and trap the blocker. Once the channel has closed, NEFA is unable to dissociate until the channel reopens. Single-channel recordings revealed that NEFA reduces the mean open time of single NMDA-activated channels in a concentration-dependent manner with a forward blocking rate (k+) of 39.9 microM-1 s-1. A computational model of antagonism by NEFA was developed and constrained using kinetic measurements of single-channel data. By multiple criteria, only models in which blocker binding in the channel causes a change in receptor operation adequately fit or predicted whole-cell data. By comparing model predictions and experimental measurements of NEFA action at a high NMDA concentration, we determined that NEFA affects receptor operation through an influence on channel gating. We conclude that inhibition of NMDA receptors by PCP-like blockers involves a modification of channel gating as well as block of current flow through the open channel.
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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.