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- W2016859575 abstract "Cis- and trans-2,4-methanoglutamate were compared with L-glutamate as acidic amino acid ligands. Cis-2,4-methanoglutamate had a Ki of 0.052 μM against N-methyl-D-aspartate (NMDA)-specific L-[3H]glutamate binding compared with 0.050 μM for L-glutamate. Cis-2,4-methanoglutamate exhibited no significant affinity against [3H]kainate or [3H]α-amino-3-hydroxy-5-methyl-4-isoxazole propionate ([3H]AMPA) binding. Trans-2,4-methanoglutamate had no significant affinity for any of these sites. Cis-2,4-methanoglutamate increased [3H]N-1[2-thienyl]cyclohexyl-3, 4-piperidine ([3H]TCP) binding with EC50 of 0.35 ± 0.14 μM. It produced an inward current in rat brain mRNA-injected Xenopus oocytes which was blocked by the NMDA antagonist, D-2-amino-7-phosphonoheptanoate (D-AP7). Cis-2,4-methanoglutamate (EC50 = 15.9 μM) was 100-fold more potent than L-glutamate (EC50 = 1,584 μM) in reducing the excitatory postsynaptic potential in CA1 of hippocampal slices. Cis-2,4-methanoglutamate is the most potent, selective NMDA agonist known." @default.
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- W2016859575 title "cis-2,4-methanoglutamate is a potent and selective N-methyl-D-aspartate receptor agonist" @default.
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- W2016859575 doi "https://doi.org/10.1016/0014-2999(90)90036-6" @default.
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