Abstract
1. Mature in vitro rat spinal cord preparations have been used to compare the depressant effects of 6-cyano-2,3-dihydroxy-7-nitroquinoxalinedione (CNQX) and kynurenate on transmission from low threshold myelinated primary afferents in dorsal roots. EC50 values +/- s.e.mean (number of preparations in parentheses) for depression of the monosynaptic ventral root reflex were respectively 1.0 +/- 0.3 microM (5) and 135 +/- 15 microM (3) for CNQX and kynurenate. Transmission through superior cervical ganglia was not significantly affected by concentrations of CNQX up to 100 microM or kynurenate up to 5 mM. 2. Immature in vitro rat spinal cord preparations were used to measure dose-ratios for antagonism of depolarizations induced by N-methyl-D-aspartate (NMDA), kainate or quisqualate by 4, 10 and 25 microM CNQX. In the presence of 0.75 mM Mg2+ pA2 values +/- s.e.mean were respectively 4.62 +/- 0.05 (16), 5.79 +/- 0.01 (4) and 5.59 +/- 0.05 (16) for each agonist. These values were not significantly altered in the absence of added Mg2+. The mean pA2 values for kainate were significantly higher than those for quisqualate (P less than 0.01). 3. Antagonism of NMDA-induced depolarizations was evident at 10 and 25 but not 4 microM CNQX. The antagonism of NMDA was reversed by D-serine (100 and 200 microM). 4. A similarity between the relative potencies of both CNQX and kynurenate for depression of synaptic transmission and antagonism of amino acid-induced depolarizations indicates that monosynaptic transmission from myelinated primary afferents to motoneurones is mediated by kainate and/or quisqualate sub-types of non-NMDA receptors.
MeSH Terms
6-Cyano-7-nitroquinoxaline-2,3-dione
Animals
Ganglia, Spinal/drug effects
Hexamethonium Compounds/pharmacology
In Vitro Techniques
Kainic Acid/pharmacology
Motor Neurons/drug effects
N-Methylaspartate/pharmacology
Quinoxalines/pharmacology
Quisqualic Acid/pharmacology
Rats
Synapses/drug effects
Tetrodotoxin/pharmacology
Chemicals
Hexamethonium Compounds
Quinoxalines
Tetrodotoxin
N-Methylaspartate
6-Cyano-7-nitroquinoxaline-2,3-dione
Quisqualic Acid
Kainic Acid
Authors & Affiliations
4 authors, click to expand affiliations / ORCID
Long S K
Duphar B.V., Weesp, Holland.
Smith D A
Siarey R J
Evans R H
References (17)
17 references, click to expand
-
The effects of a series of omega-phosphonic alpha-carboxylic amino acids on electrically evoked and excitant amino acid-induced responses in isolated spinal cord preparations.
Br J Pharmacol. 1982 Jan;75(1):65-75
PMID: 7042024
-
Kynurenic acid inhibits synaptic and acidic amino acid-induced responses in the rat hippocampus and spinal cord.
Brain Res. 1983 Aug 22;273(1):170-4
PMID: 6311346
-
Ia afferent excitation of motoneurones in the in vitro new-born rat spinal cord is selectively antagonized by kynurenate.
J Physiol. 1986 Jan;370:515-30
PMID: 2870179
-
Glycine potentiates the NMDA response in cultured mouse brain neurons.
Nature. 1987 Feb 5-11;325(6104):529-31
PMID: 2433595
-
A comparison of excitatory amino acid antagonists acting at primary afferent C fibres and motoneurones of the isolated spinal cord of the rat.
Br J Pharmacol. 1987 Jul;91(3):531-7
PMID: 3038242
-
The pharmacological selectivity of three NMDA antagonists.
Eur J Pharmacol. 1988 Jan 5;145(1):81-6
PMID: 2894999
-
An in vitro mature spinal cord preparation from the rat.
Neuropharmacology. 1988 May;27(5):541-6
PMID: 3393270
-
CNQX blocks acidic amino acid induced depolarizations and synaptic components mediated by non-NMDA receptors in rat hippocampal slices.
Neurosci Lett. 1988 Jun 29;89(2):182-6
PMID: 2899308
-
Quinoxalinediones: potent competitive non-NMDA glutamate receptor antagonists.
Science. 1988 Aug 5;241(4866):701-3
PMID: 2899909
-
7-Chlorokynurenic acid is a selective antagonist at the glycine modulatory site of the N-methyl-D-aspartate receptor complex.
Proc Natl Acad Sci U S A. 1988 Sep;85(17):6547-50
PMID: 2842779
-
Neurobiology. Quisqualate receptor antagonists.
Nature. 1988 Oct 20;335(6192):669-70
PMID: 2845277
-
Two classes of N-methyl-D-aspartate recognition sites: differential distribution and differential regulation by glycine.
Proc Natl Acad Sci U S A. 1988 Dec;85(24):9836-40
PMID: 2904680
-
6,7-Dinitro-quinoxaline-2,3-dion and 6-nitro,7-cyano-quinoxaline-2,3-dion antagonise responses to NMDA in the rat spinal cord via an action at the strychnine-insensitive glycine receptor.
Eur J Pharmacol. 1988 Oct 26;156(1):177-80
PMID: 2905271
-
Quinoxalinediones selectively block quisqualate and kainate receptors and synaptic events in rat neocortex and hippocampus and frog spinal cord in vitro.
Br J Pharmacol. 1988 Oct;95(2):585-97
PMID: 2906560
-
Glycine enhances NMDA-receptor mediated synaptic potentials in neocortical slices.
Nature. 1989 Mar 30;338(6214):422-4
PMID: 2538754
-
6-Cyano-7-nitroquinoxaline-2,3-dione as an excitatory amino acid antagonist in area CA1 of rat hippocampus.
Br J Pharmacol. 1989 May;97(1):71-6
PMID: 2566354
-
Activation of the glycine site in the NMDA receptor is necessary for the induction of LTP.
Neurosci Lett. 1990 Jan 22;108(3):261-6
PMID: 2154725