Z0877
佐替平
别名:
2-[(8-chlorodibenzo[b,f]-thiepin-10-yl)oxy]-N,N-dimethylethanamine
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关于此项目
经验公式（希尔记法）:
C18H18ClNOS
化学文摘社编号:
分子量:
331.86
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
InChI
1S/C18H18ClNOS/c1-20(2)9-10-21-16-11-13-5-3-4-6-17(13)22-18-8-7-14(19)12-15(16)18/h3-8,11-12H,9-10H2,1-2H3
SMILES string
CN(C)CCOC1=Cc2ccccc2Sc3ccc(Cl)cc13
InChI key
HDOZVRUNCMBHFH-UHFFFAOYSA-N
assay
>98% (HPLC)
form
powder
color
white to off-white
solubility
DMSO: ≥20 mg/mL
originator
Astellas
storage temp.
room temp
Quality Level
Application
Zotepine has been used as an anti-psychotic agent:
- in biophysical studies with serotonin 2A receptor (5-HT2AR)
- to study its effects on the inhibition of human organic cation transporter 1 (hOCT1)
- to study its protective effects on the human embryonic kidney (HEK cells)
Biochem/physiol Actions
Zotepine acts as an antagonist of dopamine D1, D2, and serotonin (5-HT2A/2C) receptors, and noradrenaline transporters. It shows therapeutic effects against schizophrenia and acute mania.
Zotepine is an atypical antipsychotic.
Features and Benefits
This compound is featured on the Dopamine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Astellas. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Aquatic Acute 1 - Aquatic Chronic 1
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Hung-Yu Chan et al.
Psychiatry and clinical neurosciences, 64(2), 162-169 (2010-05-08)
Atypical antipsychotics are increasingly used in the management of acute mania. This study was conducted to investigate the efficacy and tolerability of zotepine compared to haloperidol in combination with a mood stabilizer (lithium or valproate) for treatment of acute mania.
Ben Green
Expert opinion on drug metabolism & toxicology, 5(2), 181-186 (2009-02-10)
Zotepine is a second generation antipsychotic drug, a substituted dibenzothiepine tricyclic molecule, with effects on dopamine, serotonin and noradrenaline receptors. This article reviews the relevant research studies on the drug based on a search of numerous medical databases for research
Allyson V McCormick et al.
Biological psychiatry, 73(5), 464-471 (2012-11-13)
Tauopathies, including Alzheimer's disease and frontotemporal dementia, are diseases characterized by the formation of pathological tau protein aggregates in the brain and progressive neurodegeneration. Presently no effective disease-modifying treatments exist for tauopathies. To identify drugs targeting tau neurotoxicity, we have
S Yamamura et al.
British journal of pharmacology, 157(4), 656-665 (2009-04-18)
The atypical antipsychotic drug, zotepine, is effective in treatment of schizophrenia and acute mania, but the incidence of seizures during treatment is higher than with other antipsychotics. In addition, the mechanisms underlying the clinical actions of zotepine remain uncharacterized. The
Claudia Asenjo Lobos et al.
The Cochrane database of systematic reviews, (11)(11), CD006633-CD006633 (2010-11-12)
Clozapine is an atypical antipsychotic demonstrated to be superior in the treatment of refractory schizophrenia which causes fewer movement disorders. Clozapine, however, entails a significant risk of serious blood disorders such as agranulocytosis which could be potentially fatal. Currently there
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