Glycine reverses 7-chlorokynurenic acid-induced inhibition of [3H]MK-801 binding

Ratna Sircar; Mark J. Frusciante; Daniel C. Javiet; Stephen R. Zukin

doi:10.1016/0006-8993(89)91378-4

Glycine reverses 7-chlorokynurenic acid-induced inhibition of [³H]MK-801 binding

Ratna Sircar, Mark J. Frusciante, Daniel C. Javiet, Stephen R. Zukin

Research output: Contribution to journal › Article › peer-review

Abstract

7-Chlorokynurenic acid (7-Cl KYNA) has been reported to attenuate N-methyl-d-aspartate (NMDA) receptor functioning by a potent and selective inhibitory action mediated at the strychnine-insensitive glycine recognition site of the NMDA complex. Here we report that 7-Cl KYNA dose-dependently inhibits [³H]MK-801 binding to the PCP receptor, and that this effect is reversed by addittion of glycine. Since [³H]MK-801 binding is a measure of channel activation, our results are consistents with the hypothesis that 7-Cl KYNA exerts its NMDA receptor antagonism by acting at the glycine site, and that activation of the glycine site is required for NMDA channel activity to occur.

Original language	English (US)
Pages (from-to)	325-327
Number of pages	3
Journal	Brain Research
Volume	504
Issue number	2
DOIs	https://doi.org/10.1016/0006-8993(89)91378-4
State	Published - Dec 18 1989
Externally published	Yes

Keywords

7-Chlorokynurenic acid
Glycine receptor antagonist
N-methyl-d-aspartate receptor
Phencyclidine receptor
[H]MK-801 binding

ASJC Scopus subject areas

Developmental Biology
Molecular Biology
Clinical Neurology
Neuroscience(all)

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title = "Glycine reverses 7-chlorokynurenic acid-induced inhibition of [3H]MK-801 binding",

abstract = "7-Chlorokynurenic acid (7-Cl KYNA) has been reported to attenuate N-methyl-d-aspartate (NMDA) receptor functioning by a potent and selective inhibitory action mediated at the strychnine-insensitive glycine recognition site of the NMDA complex. Here we report that 7-Cl KYNA dose-dependently inhibits [3H]MK-801 binding to the PCP receptor, and that this effect is reversed by addittion of glycine. Since [3H]MK-801 binding is a measure of channel activation, our results are consistents with the hypothesis that 7-Cl KYNA exerts its NMDA receptor antagonism by acting at the glycine site, and that activation of the glycine site is required for NMDA channel activity to occur.",

keywords = "7-Chlorokynurenic acid, Glycine receptor antagonist, N-methyl-d-aspartate receptor, Phencyclidine receptor, [H]MK-801 binding",

author = "Ratna Sircar and Frusciante, {Mark J.} and Javiet, {Daniel C.} and Zukin, {Stephen R.}",

year = "1989",

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T1 - Glycine reverses 7-chlorokynurenic acid-induced inhibition of [3H]MK-801 binding

AU - Sircar, Ratna

AU - Frusciante, Mark J.

AU - Javiet, Daniel C.

AU - Zukin, Stephen R.

PY - 1989/12/18

Y1 - 1989/12/18

N2 - 7-Chlorokynurenic acid (7-Cl KYNA) has been reported to attenuate N-methyl-d-aspartate (NMDA) receptor functioning by a potent and selective inhibitory action mediated at the strychnine-insensitive glycine recognition site of the NMDA complex. Here we report that 7-Cl KYNA dose-dependently inhibits [3H]MK-801 binding to the PCP receptor, and that this effect is reversed by addittion of glycine. Since [3H]MK-801 binding is a measure of channel activation, our results are consistents with the hypothesis that 7-Cl KYNA exerts its NMDA receptor antagonism by acting at the glycine site, and that activation of the glycine site is required for NMDA channel activity to occur.

AB - 7-Chlorokynurenic acid (7-Cl KYNA) has been reported to attenuate N-methyl-d-aspartate (NMDA) receptor functioning by a potent and selective inhibitory action mediated at the strychnine-insensitive glycine recognition site of the NMDA complex. Here we report that 7-Cl KYNA dose-dependently inhibits [3H]MK-801 binding to the PCP receptor, and that this effect is reversed by addittion of glycine. Since [3H]MK-801 binding is a measure of channel activation, our results are consistents with the hypothesis that 7-Cl KYNA exerts its NMDA receptor antagonism by acting at the glycine site, and that activation of the glycine site is required for NMDA channel activity to occur.

KW - 7-Chlorokynurenic acid

KW - Glycine receptor antagonist

KW - N-methyl-d-aspartate receptor

KW - Phencyclidine receptor

KW - [H]MK-801 binding

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