摘要：

Excessive release of glutamate, a potent excitatory neurotransmitter, is thought to play an important role in a variety of acute and chronic neurological disorders, suggesting that excitatory amino acid antagonists may have broad therapeutic potential in neurology. Here, we describe the synthesis, pharmacological properties and neuroprotective activity of 9-carboxymethyl-imidazo-[1-2]indeno[1-2]pyrazin-4-one-2-carboxylic acid (=18 nM) for AMPA receptors and competitive inhibition of electrophysiological responses mediated by AMPA receptors heterologously expressed in =5 nM) and native receptors in rat brain slices (IC=0.36 μM). In in vivo testing, The synthesis and biological evaluation of original 9-carboxymethyl-5,10-imidazo[1,2-]indeno[1,2-] pyrazin-4-one-2-carboxylic acid RPR117824 is described.

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