dimetotiazine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
1235 7456-24-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • dimetotiazine mesilate
  • fonazine mesylate
  • fonazine
  • dimethiotazine
  • dimethothiazine
  • dimetotiazine
has considerable antiemetic & serotonin antagonistic action used mainly in allergic skin conditions; minor descriptor (75-84); on-line & Index Medicus search PHENOTHIAZINES (75-84); RN given refers to parent cpd
  • Molecular weight: 391.55
  • Formula: C19H25N3O2S2
  • CLOGP: 3.23
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 0
  • TPSA: 43.86
  • ALOGS: -3.78
  • ROTB: 4

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.607 Moderate 0.67
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.847 Moderate 0.67
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 26.182 10^-6 cm/s Moderate 0.67
dh-clint Dog hepatocyte intrinsic clearance 52.723 uL/min/10^6 cells Moderate 0.67
dppb Dog plasma protein binding (% unbound) 13.380 % Moderate 0.67
fcs-ppb Fetal calf serum protein binding (% unbound) 25.530 % Moderate 0.67
herg hERG pIC50 5.917 pIC50 Moderate 0.67
hh-clint Human hepatocyte intrinsic clearance 14.689 uL/min/10^6 cells Moderate 0.67
hlm-clint Human liver microsomal intrinsic clearance 104.713 uL/min/mg protein Moderate 0.67
hppb Human plasma protein binding (% unbound) 12.730 % Moderate 0.67
kinase-safety-class ACVR2B,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MET,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TTK,ZAP70 42
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 1.514 Moderate 0.67
mh-clint Mouse hepatocyte intrinsic clearance 200.909 Moderate 0.67
mppb Mouse plasma protein binding (% unbound) 11.840 Moderate 0.67
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 8.570 Moderate 0.67
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 Moderate 0.67
pppb Pig plasma protein binding (% unbound) 34.160 % Moderate 0.67
rh-clint Rat hepatocyte intrinsic clearance 279.898 uL/min/10^6 cells Moderate 0.67
rh-fuinc Rat hepatocyte fraction unbound in incubation 51.380 % Moderate 0.67
rppb Rat plasma protein binding (% unbound) 12.300 % Moderate 0.67
solubility-dd Solubility at pH 7.4 in DMSO 608.135 uM Moderate 0.67

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N02CX05 NERVOUS SYSTEM
ANALGESICS
ANTIMIGRAINE PREPARATIONS
Other antimigraine preparations
MeSH PA D006633 Histamine Antagonists
MeSH PA D006634 Histamine H1 Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018494 Histamine Agents

Related Drugs by ATC class:

N02CX Other antimigraine preparations 4 drugs
clonidineiprazochromeoxetoronepizotifen

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

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.19 Basic
pKa2 3.06 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
D07854 KEGG_DRUG
13115-40-7 SECONDARY_CAS_RN
C0118092 UMLSCUI
CHEBI:748638 CHEBI
CHEMBL346977 ChEMBL_ID
CHEMBL2104669 ChEMBL_ID
DB08967 DRUGBANK_ID
C100113 MESH_SUPPLEMENTAL_RECORD_UI
3089 PUBCHEM_CID
50138 RXNORM
003519 NDDF
003520 NDDF
B28V86NGNK UNII
2034 INN_ID
B28V86NGNK INXIGHT DRUGS

Pharmaceutical products:

None