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

Stem definitionDrug idCAS RN
1222 1841-19-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fluspirilene
  • fluspirilen
  • fluspiriline
  • redeptin
  • R 6218
  • R-6218
A long-acting injectable antipsychotic agent used for chronic schizophrenia.
  • Molecular weight: 475.58
  • Formula: C29H31F2N3O
  • CLOGP: 5.42
  • LIPINSKI: 1
  • HAC: 4
  • HDO: 1
  • TPSA: 35.58
  • ALOGS: -5.45
  • ROTB: 7

Drug dosage:

DoseUnitRoute
0.70 mg P

ADMET properties:

None

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AG01 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Diphenylbutylpiperidine 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
Schizophrenia indication 58214004 DOID:5419

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.57 acidic
pKa2 8.44 Basic
pKa3 3.93 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
Beta-2 adrenergic receptor GPCR Ki 6.29 PDSP
D(3) dopamine receptor GPCR Ki 8.41 PDSP
5-hydroxytryptamine receptor 1B GPCR Ki 5.95 PDSP
D(4) dopamine receptor GPCR Ki 8.06 PDSP
Alpha-2C adrenergic receptor GPCR Ki 7.21 PDSP
Alpha-2B adrenergic receptor GPCR Ki 7.32 PDSP
D(2) dopamine receptor GPCR Ki 9.44 PDSP
Alpha-2A adrenergic receptor GPCR Ki 6.24 PDSP
Beta-1 adrenergic receptor GPCR Ki 6.23 PDSP
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 8 IUPHAR
Histamine H1 receptor GPCR ANTAGONIST Ki 7.90 IUPHAR
5-hydroxytryptamine receptor 1A GPCR ANTAGONIST Ki 7.20 IUPHAR
5-hydroxytryptamine receptor 1D GPCR ANTAGONIST Ki 6 IUPHAR
5-hydroxytryptamine receptor 1E GPCR ANTAGONIST Ki 5.60 IUPHAR
Nociceptin receptor GPCR Ki 6.30 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.64 CHEMBL
5-hydroxytryptamine receptor 2B GPCR Ki 6.82 CHEMBL
5-hydroxytryptamine receptor 6 GPCR Ki 5.93 CHEMBL
Glycine receptor subunit alpha-1 Ion channel EC50 5.92 CHEMBL

External reference:

IDSource
N0000167366 NUI
D02629 KEGG_DRUG
C0016383 UMLSCUI
CHEBI:93369 CHEBI
CHEMBL46516 ChEMBL_ID
DB04842 DRUGBANK_ID
D005484 MESH_DESCRIPTOR_UI
85 IUPHAR_LIGAND_ID
1801 INN_ID
C5QA4GLR9M UNII
3396 PUBCHEM_CID
4507 RXNORM
003485 NDDF
321692003 SNOMEDCT_US
419373008 SNOMEDCT_US

Pharmaceutical products:

None