bromperidol ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antipsychotics, haloperidol derivatives 407 10457-90-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • bromperidol hydrochloride
  • bromperidol HCl
  • tesoprel
  • bromperidol
  • azurene
  • bromoperidol
  • impromen
bromine-substituted for chlorine in haloperidol; RN given refers to unlabeled parent cpd; structure
  • Molecular weight: 420.32
  • Formula: C21H23BrFNO2
  • CLOGP: 4
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 40.54
  • ALOGS: -4.76
  • ROTB: 6

Drug dosage:

DoseUnitRoute
10 mg O
10 mg P
3.30 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.09 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 1.98 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1973 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AD06 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Butyrophenone derivatives
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

Drug Use (View source of the data)

None




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.36 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 8.43 WOMBAT-PK KEGG DRUG
Sigma non-opioid intracellular receptor 1 Membrane receptor EC50 9.02 WOMBAT-PK
Alpha-1A adrenergic receptor GPCR Ki 7.10 WOMBAT-PK
D(3) dopamine receptor GPCR Ki 7.50 WOMBAT-PK
Histamine H1 receptor GPCR Ki 6.16 WOMBAT-PK
Muscarinic acetylcholine receptor M1 GPCR Ki 5.12 PDSP
Muscarinic acetylcholine receptor M2 GPCR Ki 5.75 PDSP
Muscarinic acetylcholine receptor M3 GPCR Ki 5.15 PDSP
Muscarinic acetylcholine receptor M4 GPCR Ki 5.77 PDSP
Muscarinic acetylcholine receptor M5 GPCR Ki 5.32 PDSP
D(1A) dopamine receptor GPCR Ki 7 WOMBAT-PK
D(4) dopamine receptor GPCR Ki 7.80 WOMBAT-PK

External reference:

IDSource
D01101 KEGG_DRUG
19777 RXNORM
C0054138 UMLSCUI
CHEBI:31305 CHEBI
CHEMBL28218 ChEMBL_ID
DB12401 DRUGBANK_ID
C006820 MESH_SUPPLEMENTAL_RECORD_UI
2448 PUBCHEM_CID
3737 INN_ID
LYH6F7I22E UNII
006754 NDDF
725571009 SNOMEDCT_US

Pharmaceutical products:

None