Pimozide is an antipsychotic compound that displays high affinity for dopamine receptors (Kis = 2.4, 0.2, and 1.8 nM for D2, D3, and D4, respectively). It also has actions as an antagonist, inverse agonist, or channel blocker, with lower affinities, at serotonin, α-adrenergic, muscarinic cholinergic, and histamine receptors and calcium and sodium channels. Pimozide is metabolized in the liver primarily by cytochrome P450 (CYP) 3A4, but CYP2D6, an isoform known to be genetically variable, can also affect metabolism. Pimozide has diverse neuropathological applications, including in Tourette syndrome.
