Indole-2-carboxylic acid (I2CA) is a competitive antagonist of the glycine site of the NMDA receptor (K i =15 μM, 5-fluoro-I2CA) and an inhibitor of HIV-1 integrase . Indole-2-carboxylic acid is selective for the glycine site of the NMDA receptor and blocks the enhancement of NMDA receptor by competitively inhibiting the binding of glycine to the NMDA receptor . Indole-2-carboxylic acid can also inhibit the strand transfer activity of HIV-1 integrase by chelating Mg 2+ at the active site of integrase and interacting with the hydrophobic cavity. Indole-2-carboxylic acid can be used in the study of neurological diseases (such as stroke, epilepsy) and HIV-1 infection.
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