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

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

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 1.50 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 40 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 3.80 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 8.30 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 5.80 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1965 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

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
Neuroleptic malignant syndrome 110.73 102.89 28 499 24968 64473237

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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)

DiseaseRelationSNOMED_IDDOID
Antisocial behavior indication 60814007




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 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:

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

External reference:

IDSource
N0000166794 NUI
D02627 KEGG_DRUG
1373 RXNORM
C0005013 UMLSCUI
CHEBI:93403 CHEBI
CHEMBL297302 ChEMBL_ID
DB12867 DRUGBANK_ID
D001544 MESH_DESCRIPTOR_UI
16363 PUBCHEM_CID
9215 IUPHAR_LIGAND_ID
1577 INN_ID
97O6X78C53 UNII
003934 NDDF
321391002 SNOMEDCT_US
391820006 SNOMEDCT_US

Pharmaceutical products:

None