SPD-502 is a novel glutamate antagonist with potential neuroprotective properties, particularly in brain ischemia. It selectively targets the AMPA receptor , showing high affinity ( IC 50 = 0.043 μM) and competitive inhibition of AMPA-induced effects in rat cortical membranes and cultured mouse cortical neurons. In vivo, SPD-502 effectively blocks AMPA-evoked spike activity in the hippocampus after intravenous administration, significantly increasing the seizure threshold in mice and demonstrating robust protection against ischemia-induced damage to hippocampal neurons in gerbils. These findings suggest SPD-502 may be promising for studying neurodegenerative conditions associated with glutamate excitotoxicity.
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