Thiothixene

Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis = 0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis = 15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis = 3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats. Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior. Formulations containing thiothixene have been used in the treatment of schizophrenia and bipolar mania.