benperidol indications/contra

Stem definitionDrug idCAS RN
antipsychotics, haloperidol derivatives 312 2062-84-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • benperidol
  • benzoperidol
  • benzperidol
  • frenactil
  • frenactyl
  • glianimon
A butyrophenone with general properties similar to those of HALOPERIDOL. It has been used in the treatment of aberrant sexual behavior. (From Martindale, The Extra Pharmacopoeia, 30th ed, p567)
  • Molecular weight: 381.45
  • Formula: C22H24FN3O2
  • CLOGP: 3.80
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 52.65
  • ALOGS: -3.38
  • ROTB: 6

Drug dosage:

DoseUnitRoute
1.50 mg O

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1965 YEAR INTRODUCED

FDA Adverse Event Reporting System

None

Pharmacologic Action:

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SourceCodeDescription
ATC N05AD07 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 D015259 Dopamine Agents
MeSH PA D018492 Dopamine Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Antisocial behavior indication 60814007

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.93 acidic
pKa2 8.12 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sigma non-opioid intracellular receptor 1 Membrane receptor EC50 5.94 WOMBAT-PK
D(4) dopamine receptor GPCR Ki 8.70 WOMBAT-PK
D(3) dopamine receptor GPCR Ki 10.18 WOMBAT-PK
5-hydroxytryptamine receptor 2A GPCR Ki 9 WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 8.47 WOMBAT-PK
D(2) dopamine receptor GPCR Ki 10.57 WOMBAT-PK

External reference:

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IDSource
N0000166794 NUI
C0005013 UMLSCUI
D02627 KEGG_DRUG
CHEMBL297302 ChEMBL_ID
391820006 SNOMEDCT_US
N0000166794 NDFRT
1373 RXNORM
321391002 SNOMEDCT_US
003934 NDDF
97O6X78C53 UNII
1577 INN_ID
16363 PUBCHEM_CID
DB12867 DRUGBANK_ID
D001544 MESH_DESCRIPTOR_UI

Pharmaceutical products:

None