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Interaction of topiramate with glycine receptor channels

Authors
Journal
Pharmacological Research
1043-6618
Publisher
Elsevier
Publication Date
Volume
51
Issue
6
Identifiers
DOI: 10.1016/j.phrs.2005.02.021
Keywords
  • Glycine Receptors
  • Topiramate
  • Channel Block
  • Patch-Clamp
Disciplines
  • Medicine

Abstract

Abstract Glycine receptor channels are pentameric ligand-gated ion channels that respond to the application of inhibitory neurotransmitters by opening of a chloride-selective central pore. Topiramate (TPM) is a broad-spectrum antiepileptic drug used as add-on or monotherapy for focal seizures. In the present study the interaction of TPM with glycine receptor channels was studied on outside-out patches from HEK293 cells expressing α 1β glycine receptor channels. The patch clamp techniques combined with ultra fast solution exchange enabled us to investigate the kinetics of receptor channels in presence of TPM. Our study showed no agonistic or potentiating effect for TPM on glycine receptor channels. However, in presence of 1 mM glycine + 1 mM TPM, the desensitization got faster and the peak current amplitude decreased. After the end of glycine + TPM pulses, off-currents occurred, suggestive for a specific channel block mechanism.

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