ArticlePloS one2014
Perampanel inhibition of AMPA receptor currents in cultured hippocampal neurons.
Article in PloS one, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed.
- Phenytoin Derivatives as Antagonists of AMPA Receptors and Voltage-Gated Sodium Channels: A Structure-Function Study.International journal of molecular sciences · 2026Article
- Molecular mechanisms of excitotoxicity and their relevance to the pathogenesis of neurodegenerative diseases-an update.Acta pharmacologica Sinica · 2025Review
- Dual Mechanisms of the Diazepine-Benzimidazole Derivative, DAB-19, in Modulating Glutamatergic Neurotransmission.International journal of molecular sciences · 2025Article
- Positive and negative allosteric modulation of GluK2 kainate receptors by BPAM344 and antiepileptic perampanel.Cell reports · 2023Article
- Parkinson's disease, epilepsy, and amyotrophic lateral sclerosis-emerging role of AMPA and kainate subtypes of ionotropic glutamate receptors.Frontiers in cell and developmental biology · 2023Review
- Structural insights into function of ionotropic glutamate receptors.Biochemistry (Moscow) Supplement. Series A, Membrane and cell biology · 2022Article
- Structure, Function, and Pharmacology of Glutamate Receptor Ion Channels.Pharmacological reviews · 2021Review
- Differential acute impact of therapeutically effective and overdose concentrations of lithium on human neuronal single cell and network function.Translational psychiatry · 2021Article
- Oxidative Stress Underlies the Ischemia/Reperfusion-Induced Internalization and Degradation of AMPA Receptors.International journal of molecular sciences · 2021Article
- Screening for Activity Against AMPA Receptors Among Anticonvulsants-Focus on Phenytoin.Frontiers in pharmacology · 2021Article
- Perampanel reduces paroxysmal depolarizing shift and inhibitory synaptic input in excitatory neurons to inhibit epileptic network oscillations.British journal of pharmacology · 2020Article
- βAnnual review of pharmacology and toxicology · 2020Review
- Coadministration of Ketamine and Perampanel Improves Behavioral Function and Reduces Inflammation in Acute Traumatic Brain Injury Mouse Model.BioMed research international · 2020Article
- Modulation of AMPA Receptor Gating by the Anticonvulsant Drug, Perampanel.ACS medicinal chemistry letters · 2019Article
- Inhibition and assessment of the biophysical gating properties of GluA2 and GluA2/A3 AMPA receptors using curcumin derivatives.PloS one · 2019Article
- Perampanel Affects Up-Stream Regulatory Signaling Pathways of GluA1 Phosphorylation in Normal and Epileptic Rats.Frontiers in cellular neuroscience · 2019Article
- α-Actinin Anchors PSD-95 at Postsynaptic Sites.Neuron · 2018Article
- CaThe EMBO journal · 2018Article
- Role of the Ion Channel Extracellular Collar in AMPA Receptor Gating.Scientific reports · 2017Article
- Structural Bases of Noncompetitive Inhibition of AMPA-Subtype Ionotropic Glutamate Receptors by Antiepileptic Drugs.Neuron · 2016Article
Corrections and comments
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Authors and funding
4 authors.
Funding
Abstract
Perampanel is an aryl substituted 2-pyridone AMPA receptor antagonist that was recently approved as a treatment for epilepsy. The drug potently inhibits AMPA receptor responses but the mode of block has not been characterized. Here the action of perampanel on AMPA receptors was investigated by whole-cell voltage-clamp recording in cultured rat hippocampal neurons. Perampanel caused a slow (τ∼1 s at 3 µM), concentration-dependent inhibition of AMPA receptor currents evoked by AMPA and kainate. The rates of block and unblock of AMPA receptor currents were 1.5×105 M-1 s-1 and 0.58 s-1, respectively. Perampanel did not affect NMDA receptor currents. The extent of block of non-desensitizing kainate-evoked currents (IC50, 0.56 µM) was similar at all kainate concentrations (3-100 µM), demonstrating a noncompetitive blocking action. Parampanel did not alter the trajectory of AMPA evoked currents indicating that it does not influence AMPA receptor desensitization. Perampanel is a selective negative allosteric AMPA receptor antagonist of high-affinity and slow blocking kinetics.
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Registered trials
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