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

Stem definitionDrug idCAS RN
1707 29216-28-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • mequitazine
  • metaplexan
  • nipolazin
  • Molecular weight: 322.47
  • Formula: C20H22N2S
  • CLOGP: 4.91
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 0
  • TPSA: 6.48
  • ALOGS: -4.91
  • ROTB: 2

Drug dosage:

DoseUnitRoute
10 mg O

ADMET properties:

None

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
Liver disorder 23.53 0 4 9 6410 2351662

FDA Adverse Event Reporting System (Male)

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

Pharmacologic Action:

SourceCodeDescription
ATC R06AD07 RESPIRATORY SYSTEM
ANTIHISTAMINES FOR SYSTEMIC USE
ANTIHISTAMINES FOR SYSTEMIC USE
Phenothiazine derivatives
MeSH PA D018494 Histamine Agents
MeSH PA D006633 Histamine Antagonists
MeSH PA D006634 Histamine H1 Antagonists
MeSH PA D018377 Neurotransmitter Agents

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.22 Basic
pKa2 3.55 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
Muscarinic acetylcholine receptor M3 GPCR Ki 8.28 PDSP
Muscarinic acetylcholine receptor M1 GPCR Ki 8.25 PDSP
Muscarinic acetylcholine receptor M5 GPCR Ki 7.96 PDSP
Histamine H1 receptor GPCR Ki 8.24 PDSP
Muscarinic acetylcholine receptor M4 GPCR Ki 7.95 PDSP
Muscarinic acetylcholine receptor M2 GPCR Ki 7.85 PDSP
Trypanothione reductase Enzyme IC50 4.66 CHEMBL
Trypanothione reductase Unclassified IC50 4.27 CHEMBL
Histamine H1 receptor GPCR Ki 8 CHEMBL

External reference:

IDSource
C0065972 UMLSCUI
D01324 KEGG_DRUG
320756004 SNOMEDCT_US
414674005 SNOMEDCT_US
29528 RXNORM
004003 NDDF
CHEMBL73451 ChEMBL_ID
DB01071 DRUGBANK_ID
CHEBI:31821 CHEBI
Y463242LY2 UNII
3672 INN_ID
4066 PUBCHEM_CID
CHEMBL1908311 ChEMBL_ID
C006069 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None