Inhibition of alpha-subunit glycine receptors by quinoxalines

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Item Type:	Article
Title:	Inhibition of alpha-subunit glycine receptors by quinoxalines
Creators Name:	Meier, J. and Schmieden, V.
Abstract:	Quinoxalines are widely used compounds in electrophysiological studies to separate excitatory and inhibitory neurotransmission mediated by the strychnine-insensitive and strychnine-sensitive glycine receptor (NMDA, GlyR), respectively. We report here, that the quinoxaline NBQX is a potent antagonist of homo-oligomeric alpha1- and alpha2-subunit glycine receptors expressed in Xenopus laevis oocytes. NBQX elicited half-maximal inhibition of glycine evoked currents at a concentration of about 5 microM. DNQX and CNQX were found to be 5-fold and 20-fold less efficient than NBQX. At oocytes expressing alpha1beta2 subunit GABAA receptors the quinoxalines tested showed no significant inhibition of GABA responses up to a concentration of 100 microM. Our data indicates that these quinoxalines applied at concentrations sufficient to block NMDA receptor also attenuate GlyR responses.
Keywords:	6-Cyano-7-nitroquinoxaline-2,3-dione, Algorithms, Drug Dose-Response Relationship, Electrophysiology, Oocytes, Quinoxalines, GABA-A Receptors, Glycine Receptors, Xenopus laevis, Animals, Frogs
Source:	NeuroReport
ISSN:	0959-4965
Publisher:	Lippincott Williams & Wilkins
Volume:	14
Number:	11
Page Range:	1507-1510
Date:	6 August 2003
Official Publication:	https://doi.org/10.1097/01.wnr.0000085903.20980.2f
PubMed:	View item in PubMed

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