pizotifen Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
2220 15574-96-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • pizotyline
  • pizotifen
  • pizotifen malate
Serotonin antagonist used against MIGRAINE DISORDERS and vascular headaches.
  • Molecular weight: 295.44
  • Formula: C19H21NS
  • CLOGP: 4.70
  • LIPINSKI: 0
  • HAC: 1
  • HDO: 0
  • TPSA: 3.24
  • ALOGS: -4.62
  • ROTB: 0

Drug dosage:

DoseUnitRoute
1.50 mg O

ADMET properties:

PropertyValueReference
BA (Bioavailability) 78 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC N02CX01 NERVOUS SYSTEM
ANALGESICS
ANTIMIGRAINE PREPARATIONS
Other antimigraine preparations
MeSH PA D000700 Analgesics
MeSH PA D018712 Analgesics, Non-Narcotic
CHEBI has role CHEBI:48279 serotonergic antagonist
CHEBI has role CHEBI:48876 muscarinic antagonist
CHEBI has role CHEBI:37956 histamine antagonist
MeSH PA D000928 Antidepressive Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D018689 Sensory System Agents
MeSH PA D018490 Serotonin Agents
MeSH PA D012702 Serotonin Antagonists

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.8 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
5-hydroxytryptamine receptor 1A GPCR ANTAGONIST Ki 7.40 IUPHAR
D(2) dopamine receptor GPCR Ki 8.62 CHEMBL
5-hydroxytryptamine receptor 7 GPCR Ki 7.60 CHEMBL
5-hydroxytryptamine receptor 2C GPCR Ki 8.85 CHEMBL
5-hydroxytryptamine receptor 2B GPCR Ki 8.70 CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 8.12 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 8.70 CHEMBL

External reference:

IDSource
N0000167169 NUI
C0032036 UMLSCUI
D05523 KEGG_DRUG
0BY8440V3N UNII
2693 INN_ID
395834002 SNOMEDCT_US
349963006 SNOMEDCT_US
8373 RXNORM
003497 NDDF
CHEBI:50212 CHEBI
CHEMBL294951 ChEMBL_ID
DB06153 DRUGBANK_ID
27400 PUBCHEM_CID
D010918 MESH_DESCRIPTOR_UI
93 IUPHAR_LIGAND_ID

Pharmaceutical products:

None