General
Preferred name
ZOTEPINE
Synonyms
Orion brand of zotepine ()
Nipolept ()
Zoleptil 25 ()
Zotepina ()
Zoleptil 50 ()
Zoleptil 100 ()
Setous ()
Zotepin ()
P&D ID
PD008996
CAS
26615-21-4
1200591-33-8
Tags
available
drug
Drug indication
Anxiety disorder
Psychosis
Drug Status
approved
withdrawn
investigational
Max Phase
2.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
INDICATION Zotepine, like other atypical antipsychotics, is considered as the first-line treatment in newly diagnosed schizophrenia. It is usually thought to be an option of choice for managing acute schizophrenic episodes when discussion with the patient is not possible. Zotepine, as an atypical antipsychotic, is used in patients who are suffering unacceptable side effects from conventional antipsychotics or in relapse patients that were inadequately controlled.[T108] ; ; It is important to consider that the indications stated above are related to atypical antipsychotics, that zotepine is not currently FDA, Canada or EMA approved and that studies have not shown any additional benefit when compared with other approved atypical antipsychotics.[A31857]; ; Schizophrenia is a chronic and severe mental disorder that affects how a person thinks, feels and behaves. It is usually marked for a loose reality perspective delineated by hallucinations, delusions and thought and movement disorders.[L1320]
DESCRIPTION Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, ¦Á1-adrenergic and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo[1][2].
PRICE 37
DESCRIPTION Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, ??1-adrenergic, and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM, and 8 nM, respectively. This second-generation antipsychotic is primarily used to treat schizophrenia, and clinical trials have investigated its efficacy as an antimanic agent in patients with acute bipolar mania.
DESCRIPTION Zotepine is an atypical antipsychotic drug, with antagonist activity at dopamine and serotonin receptors. (GtoPdb)
DESCRIPTION Zotepine is a 5-HT2A receptor and dopamine D2 receptor antagonist (Ki = 0.69 and 2.3 nM, respectively) used as an atypical antipsychotic for the treatment of schizophrenia. Zotepine also exhibits an antagonistic effect at histamine H1 receptor (IC50 = 8.0 nM). (BOC Sciences Bioactive Compounds)
DESCRIPTION Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic, and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM, and 8 nM, respectively. This second-generation antipsychotic is primarily used to treat schizophrenia, and clinical trials have investigated its efficacy as an antimanic agent in patients with acute bipolar mania. (TargetMol Bioactive Compound Library)
Compound Sets
20
BOC Sciences Bioactive Compounds
zotepine-cas-26615-21-4-item-64600
Cayman Chemical Bioactives
23909
ChEMBL Drugs
CHEMBL285802
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB09225
DrugBank Approved Drugs
DB09225
DrugCentral
2875
DrugCentral Approved Drugs
2875
DrugMAP
DMF3VXA
DrugMAP Approved Drugs
DMF3VXA
Guide to Pharmacology
103
Ki Database
ZOTEPINE
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL285802
MedChem Express Bioactive Compound Library
HY-103093
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
TargetMol Bioactive Compound Library
T19680
External IDs
34
Properties
(calculated by RDKit )
Molecular Weight
331.08
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
0
Rotatable Bonds
4
Ring Count
3
Aromatic Ring Count
2
cLogP
4.88
TPSA
12.47
Fraction CSP3
0.22
Chiral centers
0.0
Largest ring
7.0
QED
0.79
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Pathway
GPCR/G protein
Immunology/Inflammation
Neuroscience
Neuronal Signaling
Member status
member
MOA
Adrenergic receptor modulator
Dopamine D2 Antagonists
Serotonin Antagonists
dopamine receptor antagonist, serotonin receptor antagonist
Indication
schizophrenia
Target
ADRA2B, DRD2, DRD3, DRD4, HRH1, HTR1A, HTR1B, HTR1D, HTR1E, HTR2A, HTR2C, HTR6, HTR7, SLC6A2, SLC6A4
5-HT Receptor
Adrenergic Receptor
Dopamine Receptor
Histamine Receptor
5-HT2A
5-HT2C
D2
H1 receptor
α1-adrenergic receptor
Source data