Stereoselective effects of AMOA on non-NMDA receptors expressed in Xenopus oocytes

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Pharmacological characterization of the action of the novel non-N-methyl-D-aspartate (non-NMDA) antagonist AMOA (2-amino-3-[3-(carboxymethoxy)-5-methylisoxazol-4-yl]propionate) on glutamate receptors was investigated in Xenopus oocytes injected with mouse brain mRNA. AMOA (150 microM) produced a nearly parallel shift to the right of the dose-response curve for kainate-induced currents. AMOA was found to have two different effects on AMPA receptors: 1) currents elicited by low concentrations of AMPA (6 microM) were inhibited by AMOA with an IC50 value of 160 +/- 19 microM and 2) currents elicited by high concentrations of AMPA (100 microM) were potentiated with an IC50 value of 88 +/- 22 microM. The maximal potentiating effect of AMOA on AMPA currents was around 170%. Furthermore, the two opposing effects of AMOA on AMPA responses are specific for the L-configuration of AMOA. This unusual antagonistic/agonistic property of AMOA may explain its unusual properties with regard to antagonism of non-NMDA receptor-mediated events previously described.

Original languageEnglish
JournalJournal of Neuroscience Research
Issue number3
Pages (from-to)392-7
Number of pages6
Publication statusPublished - Nov 1992

    Research areas

  • Animals, Brain Chemistry, Dose-Response Relationship, Drug, Female, Ibotenic Acid, Isoxazoles, Kainic Acid, Membrane Potentials, Mice, N-Methylaspartate, Oocytes, Propionates, RNA, Messenger, Receptors, Amino Acid, Stereoisomerism, Xenopus laevis, alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid, Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, P.H.S.

ID: 171785719