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

Stem definitionDrug idCAS RN
local anaesthetics 3633 616-68-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • trimecaine
  • diethylglycinemesidide
  • mesdicain
  • mesidicaine
  • trimecain
Acetanilide derivative used as a local anesthetic.
  • Molecular weight: 248.37
  • Formula: C15H24N2O
  • CLOGP: 2.45
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 32.34
  • ALOGS: -2.70
  • ROTB: 5

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.482 Moderate 0.76
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.646 Moderate 0.76
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 33.574 10^-6 cm/s Moderate 0.76
dh-clint Dog hepatocyte intrinsic clearance 44.978 uL/min/10^6 cells Moderate 0.76
dppb Dog plasma protein binding (% unbound) 21.560 % Moderate 0.76
fcs-ppb Fetal calf serum protein binding (% unbound) 38.360 % Moderate 0.76
herg hERG pIC50 4.899 pIC50 Moderate 0.76
hh-clint Human hepatocyte intrinsic clearance 13.740 uL/min/10^6 cells Moderate 0.76
hlm-clint Human liver microsomal intrinsic clearance 37.154 uL/min/mg protein Moderate 0.76
hppb Human plasma protein binding (% unbound) 22.110 % Moderate 0.76
kinase-safety-class ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K21,MAP3K7,MAPK7,MAPK9,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK 36
kinase-selectivity-class AXL,BRAF,EIF2AK3,GRK2,PDK4 5
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 0.653 Moderate 0.70
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.489 Moderate 0.76
mh-clint Mouse hepatocyte intrinsic clearance 89.125 Moderate 0.76
mppb Mouse plasma protein binding (% unbound) 32.830 Moderate 0.76
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.514 Moderate 0.76
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 0 Moderate 0.70
pppb Pig plasma protein binding (% unbound) 39.780 % Moderate 0.76
rat-kpuu-brain Rat brain Kpuu 0.475 % Moderate 0.70
rh-clint Rat hepatocyte intrinsic clearance 110.408 uL/min/10^6 cells Moderate 0.76
rh-fuinc Rat hepatocyte fraction unbound in incubation 79.330 % Moderate 0.76
rppb Rat plasma protein binding (% unbound) 40.170 % Moderate 0.76
solubility-dd Solubility at pH 7.4 in DMSO 885.116 uM Moderate 0.76

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
MeSH PA D000777 Anesthetics
MeSH PA D000779 Anesthetics, Local
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D018689 Sensory System Agents

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 13.34 acidic
pKa2 7.92 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
D08640 KEGG_DRUG
C0041026 UMLSCUI
CHEBI:135013 CHEBI
CHEMBL1618597 ChEMBL_ID
D014288 MESH_DESCRIPTOR_UI
12028 PUBCHEM_CID
1092 INN_ID
IN1233R0JO UNII
007117 NDDF

Pharmaceutical products:

None