zotepine Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
tricyclic compounds 2875 26615-21-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • zoleptil
  • zotepine
  • lodopin
  • nipolept
  • Molecular weight: 331.86
  • Formula: C18H18ClNOS
  • CLOGP: 5.11
  • LIPINSKI: 1
  • HAC: 2
  • HDO: 0
  • TPSA: 12.47
  • ALOGS: -5.63
  • ROTB: 4

Drug dosage:

DoseUnitRoute
0.20 g O

Approvals:

None

FDA Adverse Event Reporting System

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Neuroleptic malignant syndrome 123.53 88.68 21 100 4420 3381318

Pharmacologic Action:

SourceCodeDescription
ATC N05AX11 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Other antipsychotics
CHEBI has role CHEBI:65191 second generation antipsychotic
CHEBI has role CHEBI:48539 alpha-adrenergic drug
CHEBI has role CHEBI:48278 serotonergic drug
MeSH PA D014150 Antipsychotic Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.25 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Beta-2 adrenergic receptor GPCR Ki 5.64 PDSP
Histamine H4 receptor GPCR Ki 5.70 PDSP
Alpha-1A adrenergic receptor GPCR Ki 8.15 PDSP
Sodium-dependent dopamine transporter Transporter Ki 5.44 PDSP
5-hydroxytryptamine receptor 5A GPCR Ki 7.54 PDSP
5-hydroxytryptamine receptor 3A Ion channel Ki 6.33 PDSP
Alpha-1B adrenergic receptor GPCR Ki 8.30 PDSP
Sodium-dependent serotonin transporter Transporter Ki 6.82 PDSP
Histamine H2 receptor GPCR Ki 6.30 PDSP
D(1B) dopamine receptor GPCR Ki 6.61 PDSP
Muscarinic acetylcholine receptor M3 GPCR Ki 7.14 PDSP
Alpha-2C adrenergic receptor GPCR Ki 7.02 PDSP
Alpha-2B adrenergic receptor GPCR Ki 8.27 PDSP
Muscarinic acetylcholine receptor M1 GPCR Ki 7.74 PDSP
Alpha-2A adrenergic receptor GPCR Ki 6.69 PDSP
Muscarinic acetylcholine receptor M5 GPCR Ki 6.59 PDSP
Beta-1 adrenergic receptor GPCR Ki 5.39 PDSP
Muscarinic acetylcholine receptor M2 GPCR Ki 6.85 PDSP
5-hydroxytryptamine receptor 1D GPCR ANTAGONIST Ki 9.30 IUPHAR
5-hydroxytryptamine receptor 6 GPCR ANTAGONIST Ki 8.30 IUPHAR
5-hydroxytryptamine receptor 7 GPCR ANTAGONIST Ki 8.40 IUPHAR
5-hydroxytryptamine receptor 1B GPCR ANTAGONIST Ki 7.20 IUPHAR
5-hydroxytryptamine receptor 1E GPCR ANTAGONIST Ki 6.50 IUPHAR
5-hydroxytryptamine receptor 1A GPCR Ki 6.48 CHEMBL
D(2) dopamine receptor GPCR Ki 7.96 CHEMBL
D(1A) dopamine receptor GPCR Ki 7.54 CHEMBL
D(4) dopamine receptor GPCR Ki 7.41 CHEMBL
5-hydroxytryptamine receptor 2C GPCR Ki 8.54 CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 9.04 CHEMBL
Histamine H1 receptor GPCR Ki 9.21 CHEMBL
D(3) dopamine receptor GPCR Ki 8.19 CHEMBL
Muscarinic acetylcholine receptor M4 GPCR Ki 6.26 CHEMBL
Sodium-dependent noradrenaline transporter Transporter INHIBITOR IC50 7.15 IUPHAR
5-hydroxytryptamine receptor 6 GPCR ANTAGONIST Ki 8.90 IUPHAR
5-hydroxytryptamine receptor 7 GPCR ANTAGONIST Ki 8.80 IUPHAR

External reference:

IDSource
103 IUPHAR_LIGAND_ID
C0078849 UMLSCUI
D01321 KEGG_DRUG
CHEMBL285802 ChEMBL_ID
40003 RXNORM
321641006 SNOMEDCT_US
395930007 SNOMEDCT_US
007029 NDDF
5736 PUBCHEM_CID
C022172 MESH_SUPPLEMENTAL_RECORD_UI
U29O83JAZW UNII
4112 INN_ID
DB09225 DRUGBANK_ID
CHEBI:32316 CHEBI

Pharmaceutical products:

None