zotepine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Hosey CM, Chan R, Benet LZ
BA (Bioavailability) 10 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

None

FDA Adverse Event Reporting System (Female)

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 60.89 57.13 14 345 12042 63476621

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

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 78.65 45.43 22 652 27537 79716177
Psychiatric symptom 57.22 45.43 13 661 7022 79736692
Colitis ischaemic 47.14 45.43 13 661 15346 79728368
Colectomy total 47.02 45.43 7 667 364 79743350

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AX11 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Other antipsychotics
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
CHEBI has role CHEBI:48278 serotonergic drugs
CHEBI has role CHEBI:48539 alpha-adrenergic drugs
CHEBI has role CHEBI:65191 atypical antipsychotic agent

Drug Use | Suggest Off label Use Form| |View source of the data|

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

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-1 adrenergic receptor GPCR Ki 5.39 PDSP
Beta-2 adrenergic receptor GPCR Ki 5.64 PDSP
D(1A) dopamine receptor GPCR Ki 7.54 CHEMBL
D(2) dopamine receptor GPCR Ki 7.96 CHEMBL
Alpha-2A adrenergic receptor GPCR Ki 6.69 PDSP
Sodium-dependent serotonin transporter Transporter Ki 6.82 PDSP
Sodium-dependent noradrenaline transporter Transporter INHIBITOR IC50 7.15 IUPHAR
5-hydroxytryptamine receptor 1A GPCR Ki 6.48 CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 9.04 CHEMBL
5-hydroxytryptamine receptor 2C GPCR Ki 8.54 CHEMBL
5-hydroxytryptamine receptor 6 GPCR ANTAGONIST Ki 8.30 IUPHAR
5-hydroxytryptamine receptor 7 GPCR ANTAGONIST Ki 8.40 IUPHAR
Alpha-1A adrenergic receptor GPCR Ki 8.16 PDSP
Alpha-2B adrenergic receptor GPCR Ki 8.27 PDSP
D(3) dopamine receptor GPCR Ki 8.19 CHEMBL
D(1B) dopamine receptor GPCR Ki 6.61 PDSP
Histamine H1 receptor GPCR Ki 9.21 CHEMBL
Histamine H2 receptor GPCR Ki 6.30 PDSP
Histamine H4 receptor GPCR Ki 5.70 PDSP
Muscarinic acetylcholine receptor M1 GPCR Ki 7.75 PDSP
Muscarinic acetylcholine receptor M2 GPCR Ki 6.85 PDSP
Muscarinic acetylcholine receptor M3 GPCR Ki 7.14 PDSP
Muscarinic acetylcholine receptor M4 GPCR Ki 6.26 CHEMBL
Muscarinic acetylcholine receptor M5 GPCR Ki 6.59 PDSP
5-hydroxytryptamine receptor 1B GPCR ANTAGONIST Ki 7.20 IUPHAR
5-hydroxytryptamine receptor 1D GPCR ANTAGONIST Ki 9.30 IUPHAR
Alpha-2C adrenergic receptor GPCR Ki 7.02 PDSP
Sodium-dependent dopamine transporter Transporter Ki 5.44 PDSP
D(4) dopamine receptor GPCR Ki 7.41 CHEMBL
5-hydroxytryptamine receptor 3A Ion channel Ki 6.33 PDSP
Alpha-1B adrenergic receptor GPCR Ki 8.30 PDSP
5-hydroxytryptamine receptor 5A GPCR Ki 7.54 PDSP
5-hydroxytryptamine receptor 1E GPCR ANTAGONIST Ki 6.50 IUPHAR
5-hydroxytryptamine receptor 7 GPCR ANTAGONIST Ki 8.80 IUPHAR
5-hydroxytryptamine receptor 6 GPCR ANTAGONIST Ki 8.90 IUPHAR

External reference:

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

Pharmaceutical products:

None