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thioproperazine
- Development stage
- Unknown
- Lead developer
- Sanofi
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral, Intramuscular
01
Overview
Thioproperazine is a typical antipsychotic of the phenothiazine class, specifically a phenothiazine with a piperazine side chain. It is primarily indicated for the management of acute and chronic schizophrenia, including cases refractory to other neuroleptics, and may also be used in manic syndromes. Thioproperazine acts as an antagonist at multiple postsynaptic receptors, including dopaminergic (D1, D2, D3, D4), serotonergic (5-HT1 and 5-HT2), histaminergic (H1), adrenergic (alpha1/alpha2), and muscarinic cholinergic (M1/M2) receptors. Its antipsychotic effects are mainly attributed to dopamine receptor antagonism; additional actions on serotonin and other receptors contribute to its clinical profile and side effect spectrum[1][2][3][4][7]. The drug has relatively slight sedative effects compared to some other antipsychotics[1][4].
- Brand names
- Majeptil
- Other names
- thioproperazine mesylate
02
Targets
DRD4 (Dopamine D4 Receptor)HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))HRH1 (Histamine H1 Receptor)M1 (Muscarinic acetylcholine receptor M1)ADRA2A (α2A)CHRM2 (M2)DRD1 (Dopamine D1 Receptor)ADRA1A (α1A)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)HTR1B (5-Hydroxytryptamine Receptor 1B)
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