[1][2] Xanthurenic acid is suspected to be an endogenous agonist for Group II metabotropic glutamate receptors in humans.

[3] It is also known to be a potent VGLUT inhibitor, thereby preventing the movement of glutamate from the cytoplasm into synaptic vesicles, an action that it mediates via competitive blockade of vesicular glutamate transporters (Ki = 0.19 mM).

[4] In 2015[update] researchers reported a marked reduction of xanthurenic acid levels in the serum of patients with schizophrenia.

[5] A recent meta-analysis showed that blood xanthurenic acid levels are lower in individuals suffering from bipolar disorder as well.

[6] Xanthurenic acid has also been shown to induce gametogenesis of Plasmodium falciparum, the parasite that causes malaria.