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

Stem definitionDrug idCAS RN
1214 2746-81-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fluphenazine enanthate
  • moditen enanthate
  • prolixin enanthate
  • Molecular weight: 549.70
  • Formula: C29H38F3N3O2S
  • CLOGP: 7.87
  • LIPINSKI: 2
  • HAC: 5
  • HDO: 0
  • TPSA: 36.02
  • ALOGS: -5.86
  • ROTB: 14
  • Status: OFM
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BA (Bioavailability) 2.70 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 5.238 Moderate 0.67
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.906 Moderate 0.67
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 0.203 10^-6 cm/s Moderate 0.67
dh-clint Dog hepatocyte intrinsic clearance 87.297 uL/min/10^6 cells Moderate 0.67
dppb Dog plasma protein binding (% unbound) 0.120 % Moderate 0.67
fcs-ppb Fetal calf serum protein binding (% unbound) 0.040 % Moderate 0.67
herg hERG pIC50 5.454 pIC50 Moderate 0.67
hh-clint Human hepatocyte intrinsic clearance 155.597 uL/min/10^6 cells Moderate 0.67
hlm-clint Human liver microsomal intrinsic clearance 266.073 uL/min/mg protein Moderate 0.67
hppb Human plasma protein binding (% unbound) 0.160 % Moderate 0.67
kinase-safety-class ACVR2B,AKT1,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TTK 44
kinase-selectivity-class AXL,EPHB4,PDK4 3
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.289 Moderate 0.67
mh-clint Mouse hepatocyte intrinsic clearance 198.153 Moderate 0.67
mppb Mouse plasma protein binding (% unbound) 0.240 Moderate 0.67
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.354 Moderate 0.67
pfas-class PFAS structural alert (1 = True, 0 = False) 1
pppb Pig plasma protein binding (% unbound) 0.340 % Moderate 0.67
rh-clint Rat hepatocyte intrinsic clearance 198.609 uL/min/10^6 cells Moderate 0.67
rh-fuinc Rat hepatocyte fraction unbound in incubation 0.230 % Moderate 0.67
rppb Rat plasma protein binding (% unbound) 0.110 % Moderate 0.67
solubility-dd Solubility at pH 7.4 in DMSO 0.295 uM Moderate 0.67

Approvals:

DateAgencyCompanyOrphan
March 15, 1967 FDA APOTHECON

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
FDA CS M0016525 Phenothiazines
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents
MeSH PA D014150 Antipsychotic Agents
MeSH PA D015259 Dopamine Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018492 Dopamine Antagonists
CHEBI has role CHEBI:35476 antipsychotic agent
CHEBI has role CHEBI:37930 phenothiazine antipsychotic drug
CHEBI has role CHEBI:48561 dopaminergic antagonist
CHEBI has role CHEBI:149553 anticoronaviral agent
CHEBI has role CHEBI:35469 antidepressant
CHEBI has role CHEBI:35474 anxiolytic drug
CHEBI has role CHEBI:50748 antipsoriatic
FDA EPC N0000175746 Phenothiazine

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

DiseaseRelationSNOMED_IDDOID
Schizophrenia indication 58214004 DOID:5419
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 7.85 Basic
pKa2 3.85 Basic
pKa3 2.72 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 Ki 9.27 PDSP CHEMBL
Alpha-2A adrenergic receptor GPCR Ki 6.50 PDSP
Sodium-dependent serotonin transporter Transporter Ki 5.23 PDSP
5-hydroxytryptamine receptor 1A GPCR Ki 6.84 PDSP
5-hydroxytryptamine receptor 2A GPCR Ki 7.98 PDSP
5-hydroxytryptamine receptor 2C GPCR Ki 6.05 PDSP
5-hydroxytryptamine receptor 6 GPCR Ki 7.42 PDSP
5-hydroxytryptamine receptor 7 GPCR Ki 8.10 PDSP
Alpha-1A adrenergic receptor GPCR Ki 8.19 PDSP
Alpha-2B adrenergic receptor GPCR Ki 7.09 PDSP
D(3) dopamine receptor GPCR Ki 9.61 PDSP
D(1B) dopamine receptor GPCR Ki 7.89 PDSP
Histamine H1 receptor GPCR Ki 7.68 PDSP
Histamine H2 receptor GPCR Ki 6.25 PDSP
Muscarinic acetylcholine receptor M1 GPCR Ki 5.96 PDSP
Muscarinic acetylcholine receptor M2 GPCR Ki 5.15 PDSP
Muscarinic acetylcholine receptor M3 GPCR Ki 5.84 PDSP
Muscarinic acetylcholine receptor M4 GPCR Ki 5.27 PDSP
Muscarinic acetylcholine receptor M5 GPCR Ki 6.45 PDSP
5-hydroxytryptamine receptor 1B GPCR Ki 6.48 PDSP
5-hydroxytryptamine receptor 1D GPCR Ki 6.48 PDSP
Alpha-2C adrenergic receptor GPCR Ki 7.54 PDSP
D(4) dopamine receptor GPCR Ki 7.44 PDSP
Alpha-1B adrenergic receptor GPCR Ki 7.89 PDSP
5-hydroxytryptamine receptor 5A GPCR Ki 6.84 PDSP
D(1A) dopamine receptor GPCR Ki 7.68 PDSP
5-hydroxytryptamine receptor 1E GPCR Ki 6.27 PDSP

External reference:

IDSource
4017724 VUID
N0000179195 NUI
D00792 KEGG_DRUG
4017724 VANDF
4019762 VANDF
C0066682 UMLSCUI
CHEBI:5125 CHEBI
CHEMBL1200951 ChEMBL_ID
C017610 MESH_SUPPLEMENTAL_RECORD_UI
QSB34YF0W9 UNII
3389 PUBCHEM_CID
30129 RXNORM
3882 MMSL
4749 MMSL
d00237 MMSL
001473 NDDF
001475 NDDF
111125005 SNOMEDCT_US
372730004 SNOMEDCT_US
41365009 SNOMEDCT_US
C0016368 UMLSCUI
DB00623 DRUGBANK_ID
3372 PUBCHEM_CID
946 INN_ID
D005476 MESH_DESCRIPTOR_UI
CHEBI:5123 CHEBI
QSB34YF0W9 INXIGHT DRUGS

Pharmaceutical products:

None