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Thiothixene is a typical antipsychotic.1 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.2 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.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.4 Formulations containing thiothixene have been used in the treatment of schizophrenia and bipolar mania.
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1. Research on adverse drug events. I. Muscarinic M3 receptor binding affinity could predict the risk of antipsychotics to induce type 2 diabetes. Methods Find. Exp. Clin. Pharmacol. 27(5), 289-304 (2005).
2. Drug interactions on spontaneous locomotor activity in rats. Neuroleptics and amphetamine-
3. Effects of antipsychotic drugs on latent inhibition: Sensitivity and specificity of an animal behavioral model of clinical drug action. Psychopharmacology (Berl.) 112(2-3), 315-323 (1993).
4. Submissive behavior in mice as a test for antidepressant drug activity. Pharmacol. Biochem. Behav. 82(2), 306-313 (2005).