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Perampanel Inhibition of AMPA Receptor Currents in Cultured Hippocampal Neurons
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Perampanel Inhibition of AMPA Receptor Currents in Cultured Hippocampal Neurons
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Journal Article
Perampanel Inhibition of AMPA Receptor Currents in Cultured Hippocampal Neurons
2014
Overview
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.
Publisher
Public Library of Science,Public Library of Science (PLoS)
Subject
/ Animals
/ Blocking
/ Electrophysiological Phenomena - drug effects
/ Epilepsy
/ Female
/ Glutamic acid receptors (ionotropic)
/ Kinetics
/ Ligands
/ Medicine
/ Medicine and Health Sciences
/ N-Methyl-D-aspartic acid receptors
/ Neurons
/ Rats
/ Receptors, AMPA - antagonists & inhibitors
/ Receptors, AMPA - metabolism
/ Research and Analysis Methods
/ Rodents
/ Studies
/ α-Amino-3-hydroxy-5-methyl-4-isoxazole propionic acid
/ α-Amino-3-hydroxy-5-methyl-4-isoxazole propionic acid receptors
