Indole-2-Carboxylic Acid: A Competitive Antagonist of Potentiation by Glycine at the NMDA Receptor
- 24 March 1989
- journal article
- research article
- Published by American Association for the Advancement of Science (AAAS) in Science
- Vol. 243 (4898) , 1611-1613
- https://doi.org/10.1126/science.2467381
Abstract
The N-methyl-D-aspartate (NMDA) class of excitatory amino acid receptors regulates the strength and stability of excitatory synapses and appears to play a major role in excitotoxic neuronal death associated with stroke and epilepsy. The conductance increase gated by NMDA is potentiated by the amino acid glycine, which acts at an allosteric site tightly coupled to the NMDA receptor. Indole-2-carboxylic acid (I2CA) specifically and competitively inhibits the potentiation by glycine of NMDA-gated current. In solutions containing low levels of glycine, I2CA completely blocks the response to NMDA, suggesting that NMDA alone is not sufficient for channel activation. I2CA will be useful for defining the interaction of glycine with NMDA receptors and for determining the in vivo role of glycine in excitotoxicity and synapse stabilization.This publication has 27 references indexed in Scilit:
- Requirement for Glycine in Activation of NMDA-Receptors Expressed in Xenopus OocytesScience, 1988
- Rat Brain N -Methyl-D-Aspartate Receptors Expressed in Xenopus oocytesScience, 1987
- Zinc Selectively Blocks the Action of N -Methyl-D-Aspartate on Cortical NeuronsScience, 1987
- Glycine potentiates the NMDA response in cultured mouse brain neuronsNature, 1987
- Multiple-conductance channels activated by excitatory amino acids in cerebellar neuronsNature, 1987
- Glutamate activates multiple single channel conductances in hippocampal neuronsNature, 1987
- Acidic amino acid binding sites in mammalian neuronal membranes: their characteristics and relationship to synaptic receptorsBrain Research Reviews, 1984
- Magnesium gates glutamate-activated channels in mouse central neuronesNature, 1984
- Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reactionBiochemical Pharmacology, 1973
- Drug Receptors and their FunctionNature, 1971