Building on these structural insights, we implementeda structure-baseddrug repurposing approach using an FDA-approved compound library toidentify small-molecule modulators of the NCS-1/D2R interaction.These compounds serve not only as molecular probes to investigatethe role of NCS-1 in D2R trafficking and signaling, butalso as potential therapeutic hits for the treatment of neuropsychiatricdisorders such as schizophrenia and bipolar disorder. This evidence concerns the gene DRD2 and bipolar disorder.