diphenidol indications/contra

Stem definitionDrug idCAS RN
313 972-02-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cephadol
  • difenidol
  • diphenadol
  • lansenol
  • diphenidol hydrochloride
  • diphenidol
  • difenidol hydrochloride
  • difenidol embonate
  • diphenidol HCl
  • difenidol HCl
shows anti-arrhythmic activity; RN given refers to unlabeled parent cpd
  • Molecular weight: 309.45
  • Formula: C21H27NO
  • CLOGP: 4.07
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 1
  • TPSA: 23.47
  • ALOGS: -4.72
  • ROTB: 6

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
April 5, 1967 FDA

FDA Adverse Event Reporting System

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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
Basal cell carcinoma 33.40 0 5 11 3904 3381939

Pharmacologic Action:

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SourceCodeDescription
FDA PE N0000009034 Emesis Suppression
CHEBI has role CHEBI:50919 antiemetic
MeSH PA D000932 Antiemetics
MeSH PA D001337 Autonomic Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D018373 Peripheral Nervous System Agents

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Vertigo indication 399153001

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.28 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Muscarinic acetylcholine receptor M1 GPCR ANTAGONIST Ki 7.11 DRUG MATRIX CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 6.97 DRUG MATRIX
5-hydroxytryptamine receptor 2A GPCR Ki 6.13 DRUG MATRIX
D(3) dopamine receptor GPCR Ki 6.11 DRUG MATRIX
Muscarinic acetylcholine receptor M2 GPCR Ki 6.56 DRUG MATRIX
Muscarinic acetylcholine receptor M3 GPCR Ki 7.28 DRUG MATRIX
Muscarinic acetylcholine receptor M4 GPCR Ki 7.42 DRUG MATRIX
Muscarinic acetylcholine receptor M5 GPCR Ki 6.07 DRUG MATRIX
Cytochrome P450 2D6 Enzyme IC50 6.49 DRUG MATRIX
D(2) dopamine receptor GPCR Ki 5.96 DRUG MATRIX
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel IC50 5.47 CHEMBL
Alpha-1B adrenergic receptor GPCR Ki 5.58 DRUG MATRIX

External reference:

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IDSource
C0772056 UMLSCUI
7163 IUPHAR_LIGAND_ID
D01318 KEGG_DRUG
CHEMBL936 ChEMBL_ID
4019725 VANDF
N0000147817 NDFRT
N0000007048 NDFRT
23370 RXNORM
001681 NDDF
CHEMBL1529 ChEMBL_ID
3055 PUBCHEM_CID
DG355XWQ4T UNII
3254-89-5 SECONDARY_CAS_RN
C004858 MESH_SUPPLEMENTAL_RECORD_UI
DB01231 DRUGBANK_ID
1433 INN_ID
CHEBI:4638 CHEBI

Pharmaceutical products:

None