• Neuroscience letters · Jan 2002

    Comparative Study

    Specificity of putative partial agonist, 1-aminocyclopropanecarboxylic acid, for rat N-methyl-D-aspartate receptor subunits.

    • Anton Sheinin, Rinat Nahum-Levy, Sara Shavit, and Morris Benveniste.
    • Department of Physiology and Pharmacology, Sackler School of Medicine, Tel Aviv University, Ramat Aviv 69978, Israel.
    • Neurosci. Lett. 2002 Jan 11; 317 (2): 77-80.

    AbstractThe neuroprotective compound, 1-aminocyclopropanecarboxylic acid (ACPC), has been reported to act on the N-methyl-D-aspartate (NMDA) receptors simultaneously as a glycine binding site agonist and a glutamate binding site competitive antagonist. The complex kinetics of NMDA current changes measured by a whole-cell voltage clamp in rat hippocampal neurons resulting from application and removal of 1 mM ACPC in the continual presence of 15 microM NMDA confirm this hypothesis. Two-electrode voltage clamp on Xenopus oocytes expressing NR1-1a and either NR2A, NR2B or NR2C subunits yielded biphasic ACPC dose response curves with 15 microM NMDA. NR1-1a/NR2B and NR1-1a/NR2C subunit combinations yielded overlapping dose response curves with a maximal efficacy of approximately 80%; the maximal efficacy of ACPC for the NR1-1a/NR2A subunit combination was significantly lower at approximately 60%.

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