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

Stem definitionDrug idCAS RN
psychotropics, phenylpiperazine derivatives 781 72822-12-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • dapiprazole hydrochloride
  • dapiprazole
  • AF-2139
  • dapiprazole HCl
  • Molecular weight: 325.46
  • Formula: C19H27N5
  • CLOGP: 2.03
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 0
  • TPSA: 37.19
  • ALOGS: -2.64
  • ROTB: 4

  • Status: OFM

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Dec. 31, 1990 FDA FERA PHARMS

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC S01EX02 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Other antiglaucoma preparations
MeSH PA D018663 Adrenergic Agents
FDA EPC N0000175553 alpha-Adrenergic Blocker
MeSH PA D000317 Adrenergic alpha-Antagonists
MeSH PA D018674 Adrenergic Antagonists
CHEBI has role CHEBI:37890 alpha-adrenergic antagonist
CHEBI has role CHEBI:51068 miotic
CHEBI has role CHEBI:35476 antipsychotic agent
CHEBI has role CHEBI:66981 ophthalmology drug
MeSH PA D014150 Antipsychotic Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Reverse Mydriasis from Ophthalmic Adrenergic or Anticholinergic Agent indication
Iritis contraindication 65074000 DOID:1406
Angle-closure glaucoma contraindication 392291006 DOID:13550

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.09 Basic
pKa2 5.35 Basic
pKa3 0.92 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
Alpha-1A adrenergic receptor GPCR ANTAGONIST WOMBAT-PK CHEMBL
Alpha-1D adrenergic receptor GPCR ANTAGONIST Ki 8.39 DRUG MATRIX IUPHAR
5-hydroxytryptamine receptor 2B GPCR Ki 6.17 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR Ki 6.49 DRUG MATRIX
Alpha-2B adrenergic receptor GPCR Ki 6.28 DRUG MATRIX
Alpha-1B adrenergic receptor GPCR WOMBAT-PK
5-hydroxytryptamine receptor 1A GPCR Ki 5.93 DRUG MATRIX
5-hydroxytryptamine receptor 2A GPCR Ki 6.76 DRUG MATRIX
Alpha-1B adrenergic receptor GPCR Ki 7.52 DRUG MATRIX
5-hydroxytryptamine receptor 1A GPCR IC50 5.69 CHEMBL
Alpha-1A adrenergic receptor GPCR IC50 7.02 CHEMBL

External reference:

IDSource
4020111 VUID
N0000148101 NUI
C0770916 UMLSCUI
D03648 KEGG_DRUG
5RNZ8GJO7K UNII
4983 INN_ID
108840006 SNOMEDCT_US
4020523 VANDF
22298 RXNORM
372549002 SNOMEDCT_US
003595 NDDF
DB00298 DRUGBANK_ID
72822-13-0 SECONDARY_CAS_RN
CHEBI:51066 CHEBI
7155 IUPHAR_LIGAND_ID
3033538 PUBCHEM_CID
CHEMBL1201044 ChEMBL_ID
CHEMBL1201216 ChEMBL_ID
C035289 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
DAPIPRAZOLE HUMAN PRESCRIPTION DRUG LABEL 1 53020-265 KIT 25 mg None ANDA 11 sections