blonanserin ๐Ÿถ Veterinary Use | 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: 6.73
  • 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 ยตM/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
Psychiatric symptom 81.18 48.86 16 441 5207 63483358
Salivary hypersecretion 52.80 48.86 12 445 7654 63480911
Parkinsonism 49.11 48.86 12 445 10427 63478138

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 49.29 43.41 6 283 67 34956575
Floppy iris syndrome 48.32 43.41 7 282 310 34956332

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
Psychiatric symptom 97.77 41.35 21 825 7014 79736528
Hallucination, auditory 66.18 41.35 19 827 20674 79722868
Salivary hypersecretion 54.27 41.35 15 831 14209 79729333
Procedural failure 46.50 41.35 6 840 84 79743458
Floppy iris syndrome 45.57 41.35 7 839 356 79743186
Pneumonia aspiration 44.35 41.35 19 827 66948 79676594
Parkinsonism 43.21 41.35 13 833 16571 79726971

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

None

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Schizophrenia indication 58214004 DOID:5419




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 9.05 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
D01176 KEGG_DRUG
C0287983 UMLSCUI
CHEBI:31296 CHEBI
CHEMBL178803 ChEMBL_ID
DB09223 DRUGBANK_ID
C079310 MESH_SUPPLEMENTAL_RECORD_UI
125564 PUBCHEM_CID
7670 IUPHAR_LIGAND_ID
7563 INN_ID
AQ316B4F8C UNII

Pharmaceutical products:

None