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

Stem definitionDrug idCAS RN
1712 5588-33-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • mesoridazine besilate
  • mesoridazine
  • thioridazine-2-sulfoxide
  • mesoridazine besylate
A phenothiazine antipsychotic with effects similar to CHLORPROMAZINE.
  • Molecular weight: 386.57
  • Formula: C21H26N2OS2
  • CLOGP: 4.64
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 0
  • TPSA: 23.55
  • ALOGS: -3.70
  • ROTB: 4

  • Status: OFM

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.20 g O
0.20 g P

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 10.81 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Feb. 27, 1970 FDA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AC03 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Phenothiazines with piperidine structure
FDA EPC N0000175746 Phenothiazine
FDA CS M0016525 Phenothiazines
MeSH PA D014150 Antipsychotic Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D015259 Dopamine Agents
MeSH PA D018492 Dopamine Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D011619 Psychotropic Drugs
CHEBI has role CHEBI:48561 dopaminergic antagonist
CHEBI has role CHEBI:65190 first generation antipsychotic
MeSH PA D014149 Tranquilizing Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Schizophrenia indication 58214004 DOID:5419
Hyperkalemia contraindication 14140009
Neuroleptic malignant syndrome contraindication 15244003 DOID:14464
Orthostatic hypotension contraindication 28651003
Hypokalemia contraindication 43339004
Conduction disorder of the heart contraindication 44808001
Epilepsy contraindication 84757009 DOID:1826
Stupor contraindication 89458003
Tardive dyskinesia contraindication 102449007
Prolonged QT interval contraindication 111975006
Coma contraindication 371632003
Granulocytopenic disorder contraindication 417672002
Congenital long QT syndrome contraindication 442917000
Predisposed to Torsades de Pointes Cardiac Arrhythmias contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.22 Basic
pKa2 3.45 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
D(2) dopamine receptor GPCR ANTAGONIST Ki 7.72 PDSP CHEMBL
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 8.12 PDSP CHEMBL
Histamine H1 receptor GPCR Ki 8.74 PDSP
5-hydroxytryptamine receptor 2C GPCR Ki 6.80 PDSP
D(4) dopamine receptor GPCR Ki 8.04 PDSP
Muscarinic acetylcholine receptor M3 GPCR Ki 7.05 PDSP
Muscarinic acetylcholine receptor M1 GPCR Ki 8 PDSP
Muscarinic acetylcholine receptor M5 GPCR Ki 7.22 PDSP
Muscarinic acetylcholine receptor M4 GPCR Ki 7.72 PDSP
Muscarinic acetylcholine receptor M2 GPCR Ki 7.82 PDSP
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 6.50 CHEMBL
5-hydroxytryptamine receptor 1A GPCR ANTAGONIST Ki 6.98 IUPHAR
5-hydroxytryptamine receptor 6 GPCR Ki 6.42 PDSP
D(1A) dopamine receptor GPCR ANTAGONIST Ki 6.99 IUPHAR
D(3) dopamine receptor GPCR Ki 8.59 PDSP

External reference:

IDSource
4019816 VUID
N0000147905 NUI
C0025497 UMLSCUI
D00795 KEGG_DRUG
5XE4NWM740 UNII
2019 INN_ID
78684000 SNOMEDCT_US
4019816 VANDF
6779 RXNORM
372852001 SNOMEDCT_US
d00889 MMSL
004594 NDDF
CHEMBL1088 ChEMBL_ID
C529599 MESH_SUPPLEMENTAL_RECORD_UI
DB00933 DRUGBANK_ID
32672-69-8 SECONDARY_CAS_RN
CHEBI:6780 CHEBI
CHEMBL1201052 ChEMBL_ID
D008653 MESH_DESCRIPTOR_UI
4078 PUBCHEM_CID
7227 IUPHAR_LIGAND_ID

Pharmaceutical products:

None