Abstract
A stoichiometric analysis of N-methyl-D-aspartate (NMDA) receptor binding was conducted using [3H]dizocilpine, [3H]dichlorokynurenic acid and [3H]CGP39653, and membranes from various brain regions of rats. The ratio of the density of [3H]CGP39653 binding to [3H]dizocilpine binding was > 1 in frontal cortex and hippocampus, approximately 1 in striatum and spinal cord and < 1 in cerebellum. When [3H]dichlorokynurenic acid binding was compared with [3H]dizocilpine binding, the ratios were > 1 in frontal cortex, hippocampus and striatum, 3-4 in cerebellum, and approximately 2 in spinal cord. These observations suggest that a single channel complex may have more than one binding site for NMDA and/or glycine and that the stoichiometry between the binding domains of the NMDA receptor varies regionally.
MeSH terms
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2-Amino-5-phosphonovalerate / analogs & derivatives
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2-Amino-5-phosphonovalerate / pharmacokinetics
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2-Amino-5-phosphonovalerate / pharmacology
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Animals
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Brain / anatomy & histology*
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Brain Chemistry / drug effects
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Brain Chemistry / physiology*
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Dizocilpine Maleate / pharmacokinetics
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Dizocilpine Maleate / pharmacology
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Excitatory Amino Acid Antagonists / pharmacokinetics
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Excitatory Amino Acid Antagonists / pharmacology
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In Vitro Techniques
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Kinetics
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Kynurenic Acid / analogs & derivatives
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Kynurenic Acid / pharmacokinetics
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Kynurenic Acid / pharmacology
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Male
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Nerve Tissue Proteins / metabolism
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Radioligand Assay
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Rats
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Rats, Inbred F344
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Receptors, Glycine / drug effects
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Receptors, Glycine / metabolism
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Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors
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Receptors, N-Methyl-D-Aspartate / metabolism*
Substances
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Excitatory Amino Acid Antagonists
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Nerve Tissue Proteins
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Receptors, Glycine
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Receptors, N-Methyl-D-Aspartate
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CGP 39653
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Dizocilpine Maleate
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2-Amino-5-phosphonovalerate
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Kynurenic Acid
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5,7-dichlorokynurenic acid