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

Stem definitionDrug idCAS RN
serotonin receptor antagonists (mostly 5-HT2) 388 132810-10-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • blonanserin
  • lonasen
  • AD-5423
  • Molecular weight: 367.51
  • Formula: C23H30FN3
  • CLOGP: 6.48
  • LIPINSKI: 1
  • HAC: 3
  • HDO: 0
  • TPSA: 19.37
  • ALOGS: -4.01
  • ROTB: 3

Drug dosage:

None

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.93 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Jan. 25, 2008 PMDA Dainippon Sumitomo Pharma Co., Ltd.

FDA Adverse Event Reporting System (Female)

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
Schizophrenia 77.69 45.47 18 475 8550 46677019
Psychiatric symptom 60.18 45.47 13 480 4484 46681085
Salivary hypersecretion 55.52 45.47 13 480 6432 46679137
Parkinsonism 52.81 45.47 13 480 7935 46677634

FDA Adverse Event Reporting System (Male)

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
Procedural failure 46.84 41.11 6 366 67 29952039
Floppy iris syndrome 45.37 41.11 7 365 314 29951792

Pharmacologic Action:

None

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 9.05 Basic
pKa2 5.85 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 9.85 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 9.09 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 6.54 WOMBAT-PK
Alpha-1A adrenergic receptor GPCR Ki 7.25 WOMBAT-PK

External reference:

IDSource
AQ316B4F8C UNII
D01176 KEGG_DRUG
C3179252 UMLSCUI
CHEBI:31296 CHEBI
CHEMBL178803 ChEMBL_ID
125564 PUBCHEM_CID
DB09223 DRUGBANK_ID
7563 INN_ID
C079310 MESH_SUPPLEMENTAL_RECORD_UI
7670 IUPHAR_LIGAND_ID

Pharmaceutical products:

None