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

Stem definitionDrug idCAS RN
59 2751-68-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • acetofenazine
  • acetofenazine maleate
  • acetophenazine
  • acetophenazine maleate
  • tindal
  • tindal maleate
major descriptor (73-85); minor descriptor (64-72); on-line search PHENOTHIAZINES (64-85); Index Medicus search PHENOTHIAZINES (64-72); ACETOPHENAZINE (73-85); RN given refers to parent cpd
  • Molecular weight: 411.56
  • Formula: C23H29N3O2S
  • CLOGP: 2.91
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 47.02
  • ALOGS: -3.84
  • ROTB: 7
  • Status: OFM
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
50 mg O

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.480 Moderate 0.72
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.153 Moderate 0.72
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 21.827 10^-6 cm/s Moderate 0.72
dh-clint Dog hepatocyte intrinsic clearance 48.865 uL/min/10^6 cells Moderate 0.72
dppb Dog plasma protein binding (% unbound) 12.130 % Moderate 0.72
herg hERG pIC50 5.703 pIC50 Moderate 0.72
fcs-ppb Fetal calf serum protein binding (% unbound) 21.400 % Moderate 0.72
hh-clint Human hepatocyte intrinsic clearance 19.724 uL/min/10^6 cells Moderate 0.72
hlm-clint Human liver microsomal intrinsic clearance 39.264 uL/min/mg protein Moderate 0.72
hppb Human plasma protein binding (% unbound) 8.390 % Moderate 0.72
kinase-safety-class ACVR2A,ACVR2B,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAP4K1,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 53
kinase-selectivity-class AXL,CDK4,EPHB4,PDK4,SIK2,STK33 6
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 3.741 Moderate 0.72
mh-clint Mouse hepatocyte intrinsic clearance 157.761 Moderate 0.72
mppb Mouse plasma protein binding (% unbound) 11.160 Moderate 0.72
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 11.722 Moderate 0.72
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 28.050 % Moderate 0.72
rh-clint Rat hepatocyte intrinsic clearance 154.170 uL/min/10^6 cells Moderate 0.72
rh-fuinc Rat hepatocyte fraction unbound in incubation 54.360 % Moderate 0.72
rppb Rat plasma protein binding (% unbound) 10.640 % Moderate 0.72
solubility-dd Solubility at pH 7.4 in DMSO 307.610 uM Moderate 0.72

Approvals:

DateAgencyCompanyOrphan
April 5, 1961 FDA SCHERING

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 N05AB07 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Phenothiazines with piperazine structure
CHEBI has role CHEBI:35476 antipsychotic agent
CHEBI has role CHEBI:37930 phenothiazine antipsychotic drug

Related Drugs by ATC class:

N05AB Phenothiazines with piperazine structure 9 drugs
butaperazinedixyrazinefluphenazineperazineperphenazineprochlorperazinethiopropazatethioproperazinetrifluoperazine

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

DiseaseRelationSNOMED_IDDOID
Psychotic disorder indication 69322001
Alcoholism contraindication 7200002
Organophosphate poisoning contraindication 8260003
Weight gain finding contraindication 8943002
Neuroleptic malignant syndrome contraindication 15244003 DOID:14464
Senile dementia contraindication 15662003
Chronic disease of respiratory system contraindication 17097001
Myocardial infarction contraindication 22298006 DOID:5844
Glaucoma contraindication 23986001 DOID:1686
Orthostatic hypotension contraindication 28651003
Torsades de pointes contraindication 31722008
Parkinsonism contraindication 32798002
Conduction disorder of the heart contraindication 44808001
Chronic heart failure contraindication 48447003
Bradycardia contraindication 48867003
Extrapyramidal disease contraindication 76349003
Hyperglycemia contraindication 80394007 DOID:4195
Epilepsy contraindication 84757009 DOID:1826
Leukopenia contraindication 84828003 DOID:615
Stupor contraindication 89458003
Tardive dyskinesia contraindication 102449007
Prolonged QT interval contraindication 111975006
Acute disease of cardiovascular system contraindication 128487001
Angina pectoris contraindication 194828000
Disease of liver contraindication 235856003 DOID:409
Metabolic syndrome X contraindication 237602007 DOID:14221
Hyperprolactinemia contraindication 237662005 DOID:12700
Benign prostatic hyperplasia contraindication 266569009
Retention of urine contraindication 267064002
Anemia contraindication 271737000 DOID:2355
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Neutropenic disorder contraindication 303011007 DOID:1227
Coma contraindication 371632003
At risk for aspiration contraindication 371736008
Visual impairment contraindication 397540003
Breastfeeding (mother) contraindication 413712001
Myocardial ischemia contraindication 414795007 DOID:3393
Obesity contraindication 414916001 DOID:9970
Congenital long QT syndrome contraindication 442917000
Carcinoma of female breast contraindication 447782002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.21 Basic
pKa2 4.21 Basic
pKa3 1.82 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
D(2) dopamine receptor GPCR ANTAGONIST DRUGBANK CHEMBL
Androgen receptor Transcription factor Ki 6.10 CHEMBL

External reference:

IDSource
4019593 VUID
N0000179028 NUI
D00788 KEGG_DRUG
16735 RXNORM
C0050458 UMLSCUI
CHEBI:2401 CHEBI
CHEMBL1085 ChEMBL_ID
CHEMBL2360079 ChEMBL_ID
DB01063 DRUGBANK_ID
C100162 MESH_SUPPLEMENTAL_RECORD_UI
17676 PUBCHEM_CID
1026 INN_ID
5714-00-1 SECONDARY_CAS_RN
8620H6K4QH UNII
4018806 VANDF
4019593 VANDF
001485 NDDF
004592 NDDF
35281007 SNOMEDCT_US
67029008 SNOMEDCT_US
8620H6K4QH INXIGHT DRUGS

Pharmaceutical products:

None