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

Stem definitionDrug idCAS RN
diazepam derivatives 1936 2011-67-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • nimetazepam
  • methylnitrazepam
  • nimetazam
  • Molecular weight: 295.30
  • Formula: C16H13N3O3
  • CLOGP: 1.99
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 0
  • TPSA: 78.49
  • ALOGS: -4.05
  • ROTB: 2

Drug dosage:

None

ADMET properties:

PropertyValueReference
BA (Bioavailability) 95 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.123 Moderate 0.73
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.581 Moderate 0.73
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 89.743 10^-6 cm/s Moderate 0.73
dh-clint Dog hepatocyte intrinsic clearance 38.459 uL/min/10^6 cells Moderate 0.73
dppb Dog plasma protein binding (% unbound) 21.670 % Moderate 0.73
fcs-ppb Fetal calf serum protein binding (% unbound) 36.740 % Moderate 0.73
herg hERG pIC50 4.547 pIC50 Moderate 0.73
hh-clint Human hepatocyte intrinsic clearance 4.887 uL/min/10^6 cells Moderate 0.73
hlm-clint Human liver microsomal intrinsic clearance 13.366 uL/min/mg protein Moderate 0.73
hppb Human plasma protein binding (% unbound) 21.400 % Moderate 0.73
kinase-safety-class ACVR2B,AXL,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAP3K1,MAP3K21,MAPK10,MAPK7,MARK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PRKDC,STK33,TEK,TTK 25
kinase-selectivity-class AXL,GRK2,STK33,TTK 4
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 1.340 Moderate 0.68
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.681 Moderate 0.73
mh-clint Mouse hepatocyte intrinsic clearance 48.084 Moderate 0.73
mppb Mouse plasma protein binding (% unbound) 20.980 Moderate 0.73
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.822 Moderate 0.73
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 29.040 % Moderate 0.73
rat-kpuu-brain Rat brain Kpuu 0.200 % Moderate 0.68
rh-clint Rat hepatocyte intrinsic clearance 67.143 uL/min/10^6 cells Moderate 0.73
rh-fuinc Rat hepatocyte fraction unbound in incubation 82.720 % Moderate 0.73
rppb Rat plasma protein binding (% unbound) 20.560 % Moderate 0.73
solubility-dd Solubility at pH 7.4 in DMSO 394.457 uM Moderate 0.73

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 N05CD15 NERVOUS SYSTEM
PSYCHOLEPTICS
HYPNOTICS AND SEDATIVES
Benzodiazepine derivatives
MeSH PA D000927 Anticonvulsants
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D006993 Hypnotics and Sedatives
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents
MeSH PA D014151 Anti-Anxiety Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018682 GABA Agents
MeSH PA D018757 GABA Modulators
CHEBI has role CHEBI:35623 anticonvulsant
CHEBI has role CHEBI:35717 sedative
CHEBI has role CHEBI:50268 GABA modulator
CHEBI has role CHEBI:53784 antispasmodic drug

Related Drugs by ATC class:

N05CD Benzodiazepine derivatives 14 drugs
brotizolamcinolazepamdoxefazepamestazolamflunitrazepamflurazepamloprazolamlormetazepammidazolamnitrazepamquazepamremimazolam show all 14 →

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

DiseaseRelationSNOMED_IDDOID
Insomnia indication 193462001




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.48 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
D01593 KEGG_DRUG
C0068774 UMLSCUI
CHEBI:31912 CHEBI
CHEMBL13341 ChEMBL_ID
C002714 MESH_SUPPLEMENTAL_RECORD_UI
4496 PUBCHEM_CID
3150 INN_ID
4532264KW6 UNII

Pharmaceutical products:

None