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

Stem definitionDrug idCAS RN
1640 22232-71-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • mazindol
  • mazanor
  • mazildene
Tricyclic anorexigenic agent unrelated to and less toxic than AMPHETAMINE, but with some similar side effects. It inhibits uptake of catecholamines and blocks the binding of cocaine to the dopamine uptake transporter.
  • Molecular weight: 284.74
  • Formula: C16H13ClN2O
  • CLOGP: 3.39
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 35.83
  • ALOGS: -3.31
  • ROTB: 1

  • Status: OFM

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

Drug dosage:

DoseUnitRoute
1 mg O

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.12 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 93 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
June 14, 1973 FDA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC A08AA05 ALIMENTARY TRACT AND METABOLISM
ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS
ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS
Centrally acting antiobesity products
MeSH PA D018663 Adrenergic Agents
MeSH PA D018759 Adrenergic Uptake Inhibitors
MeSH PA D002491 Central Nervous System Agents
MeSH PA D000697 Central Nervous System Stimulants
MeSH PA D015259 Dopamine Agents
MeSH PA D018765 Dopamine Uptake Inhibitors
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D014179 Neurotransmitter Uptake Inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Obesity indication 414916001 DOID:9970

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.93 acidic
pKa2 10.1 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
Sodium-dependent serotonin transporter Transporter INHIBITOR Ki 7.30 CHEMBL CHEMBL
Sodium-dependent dopamine transporter Transporter INHIBITOR Ki 8 CHEMBL CHEMBL
Sodium-dependent noradrenaline transporter Transporter INHIBITOR Kd 9.30 CHEMBL CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane receptor IC50 6.63 CHEMBL
Histamine H1 receptor GPCR Ki 6.22 PDSP
Transporter Transporter Ki 9.10 CHEMBL
Sodium-dependent serotonin transporter Transporter Ki 6.61 CHEMBL
Sodium-dependent dopamine transporter Transporter Kd 8.06 CHEMBL

External reference:

IDSource
4018025 VUID
N0000146368 NUI
C0024977 UMLSCUI
D00367 KEGG_DRUG
4194004 SNOMEDCT_US
4018025 VANDF
6664 RXNORM
387232005 SNOMEDCT_US
5025 MMSL
d00811 MMSL
001874 NDDF
C56709M5NH UNII
2895 INN_ID
CHEBI:6702 CHEBI
CHEMBL781 ChEMBL_ID
DB00579 DRUGBANK_ID
4020 PUBCHEM_CID
D008454 MESH_DESCRIPTOR_UI
4797 IUPHAR_LIGAND_ID

Pharmaceutical products:

None