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PMID: 1976402 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't

Effect of 6-cyano-2,3-dihydroxy-7-nitro-quinoxaline (CNQX) on dorsal root-, NMDA-, kainate- and quisqualate-mediated depolarization of rat motoneurones in vitro.

British journal of pharmacology ·Vol. 100 ·No. 4 ·1990-08-00 ·Pages 850-4

Long SK, Smith DA, Siarey RJ, Evans RH

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
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Article Info
Journal
British journal of pharmacology
Abbr.
Br J Pharmacol
ISSN
0007-1188
Published
1990-08-00
Pages
850-4
Language
English
Region
England
NLM ID
7502536
PMCID
PMC1917604
Subset
IM
Grants
Wellcome Trust · United Kingdom
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