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Merck

Z0877

Zotepine

Sinónimos:

2-[(8-chlorodibenzo[b,f]-thiepin-10-yl)oxy]-N,N-dimethylethanamine

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Acerca de este artículo

Fórmula empírica (notación de Hill):
C18H18ClNOS
Número CAS:
Peso molecular:
331.86
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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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.

pictograms

Exclamation markEnvironment

signalword

Warning

hcodes

Hazard Classifications

Acute Tox. 4 Oral - Aquatic Acute 1 - Aquatic Chronic 1

Clase de almacenamiento

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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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
Selvizhi Subramanian et al.
The Cochrane database of systematic reviews, (10)(10), CD006628-CD006628 (2010-10-12)
In many parts of the world, particularly in industrialised countries, second generation (atypical) antipsychotic drugs have become first line treatment for people suffering from schizophrenia. The question as to whether the effects of various second generation antipsychotic drugs differ is
Kazuyoshi Nozaki et al.
Analytical sciences : the international journal of the Japan Society for Analytical Chemistry, 25(10), 1197-1201 (2009-10-14)
A simple, rapid, and sensitive on-line liquid chromatographic electrochemistry/electrospray/tandem mass spectrometry (LC-EC/ESI-MS/MS) method for the determination of zotepine in human serum was developed using a new generated-electrochemically fragment ion, and was validated. A recent novel technique of LC-EC/ESI-MS/MS that combines
Britta Haenisch et al.
Naunyn-Schmiedeberg's archives of pharmacology, 385(10), 1017-1023 (2012-07-19)
Besides the three antidepressant-sensitive, Na(+)- and Cl(-)-dependent monoamine transporters, Na(+)-independent organic cation transporters (OCTs) are known to transport monoamines. However, little is known about the interactions of psychotropic drugs with human (h) OCTs. In the present study, a series of

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