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

Stem definitionDrug idCAS RN
903 5636-83-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • dimetindene maleate
  • dimethindene maleate
  • dimethindene
  • dimetindene
A histamine H1 antagonist. It is used in hypersensitivity reactions, in rhinitis, for pruritus, and in some common cold remedies.
  • Molecular weight: 292.43
  • Formula: C20H24N2
  • CLOGP: 3.53
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 0
  • TPSA: 16.13
  • ALOGS: -3.88
  • ROTB: 5

Drug dosage:

DoseUnitRoute
4 mg O

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 2.16 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 4.83 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 4.60 hours Lombardo F, Berellini G, Obach RS

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC D04AA13 DERMATOLOGICALS
ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC.
ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC.
Antihistamines for topical use
ATC R06AB03 RESPIRATORY SYSTEM
ANTIHISTAMINES FOR SYSTEMIC USE
ANTIHISTAMINES FOR SYSTEMIC USE
Substituted alkylamines
MeSH PA D018926 Anti-Allergic Agents
MeSH PA D000982 Antipruritics
MeSH PA D003879 Dermatologic Agents
MeSH PA D018494 Histamine Agents
MeSH PA D006633 Histamine Antagonists
MeSH PA D006634 Histamine H1 Antagonists
MeSH PA D018377 Neurotransmitter Agents

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.21 Basic
pKa2 5.05 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
Muscarinic acetylcholine receptor M2 GPCR Ki 7.35 CHEMBL
Muscarinic acetylcholine receptor M4 GPCR Ki 6.39 CHEMBL
Muscarinic acetylcholine receptor M5 GPCR Ki 6.10 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 6.58 CHEMBL
Muscarinic acetylcholine receptor M3 GPCR Ki 6.72 CHEMBL
Histamine H1 receptor GPCR Ki 9.16 CHEMBL

External reference:

IDSource
D004115 MESH_DESCRIPTOR_UI
C0813204 UMLSCUI
D01343 KEGG_DRUG
661FH77Z3P UNII
1403 INN_ID
3614-69-5 SECONDARY_CAS_RN
26122009 SNOMEDCT_US
3449 RXNORM
387142004 SNOMEDCT_US
004804 NDDF
CHEBI:135222 CHEBI
CHEMBL22108 ChEMBL_ID
DB08801 DRUGBANK_ID
10101 IUPHAR_LIGAND_ID
21855 PUBCHEM_CID
CHEMBL1870768 ChEMBL_ID

Pharmaceutical products:

None