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thiothixene
- Development stage
- Approved
- Lead developer
- Pfizer
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Thiothixene is a first-generation (typical) antipsychotic medication belonging to the thioxanthene class. It is primarily indicated for the treatment of schizophrenia, both acute and chronic, and may also be used in other psychiatric disorders such as bipolar disorder, mania, and behavioral disturbances[1][4][5]. Thiothixene acts mainly by antagonizing dopamine receptors (D1, D2, D3, D4), thereby reducing abnormal excitement in the brain and balancing dopamine levels to help regulate mood, behavior, and thoughts[1][2][3][6]. It also exhibits antagonistic activity at serotonergic (5-HT1 and 5-HT2), histaminergic (H1), alpha-adrenergic (alpha1/alpha2), and muscarinic cholinergic (M1/M2) receptors[3][6]. These actions contribute to its antipsychotic effects as well as its side effect profile. The drug is administered orally; it is rapidly absorbed with peak plasma concentrations within 1–3 hours after dosing. Thiothixene was originally developed by pharmaceutical companies such as Pfizer.
- Brand names
- Navane
- Other names
- tiotixene
02
Targets
HTR2A (Serotonin receptor 5-HT2A)DRD4 (Dopamine D4 Receptor)ADRA1A (α1A)HRH1 (Histamine H1 Receptor)mAChR (Muscarinic acetylcholine receptors)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))DRD1 (Dopamine D1 Receptor)DRD2 (Dopamine D2 Receptor)HTR2C (5-hydroxytryptamine 2C receptor)DRD3 (Dopamine receptor D3)
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