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trifluperidol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antipsychotics, haloperidol derivatives | 2741 | 749-13-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A butyrophenone with general properties similar to those of HALOPERIDOL. It is used in the treatment of PSYCHOSES including MANIA and SCHIZOPHRENIA. (From Martindale, The Extra Pharmacopoeia, 30th ed, p621)
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 2 | mg | O |
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.309 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.826 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 26.915 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 14.928 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 8.410 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 26.640 | % | High | 1 |
| herg | hERG pIC50 | 6.528 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 5.070 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 32.434 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 8.410 | % | High | 1 |
| kinase-safety-class | ACVR2B,AKT1,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAP3K7,MAPK10,MAPK12,MAPK7,MET,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIM2,PRKDC,SIK2,SIK3,TEK,TGFBR1 | 33 | |||
| kinase-selectivity-class | AKT3,AXL,EIF2AK3,EPHB4,PDK4,PRKCD,SIK2 | 7 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.741 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 33.420 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 9.300 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 2.168 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 1 | |||
| pppb | Pig plasma protein binding (% unbound) | 19.310 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 84.918 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 22.110 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 9.130 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 192.752 | uM | High | 1 |
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:
| Source | Code | Description |
|---|---|---|
| ATC | N05AD02 | NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Butyrophenone derivatives |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D011619 | Psychotropic Drugs |
| 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 |
Related Drugs by ATC class:
N05AD Butyrophenone derivatives 8 drugs
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 level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.36 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| D(3) dopamine receptor | GPCR | Ki | 8.46 | PDSP | |||||
| D(4) dopamine receptor | GPCR | Ki | 9.46 | PDSP | |||||
| D(2) dopamine receptor | GPCR | Ki | 9.70 | PDSP | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 9.08 | CHEMBL | |||||
| 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase | Enzyme | Ki | 6.78 | CHEMBL | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 9.10 | CHEMBL | |||||
| C-8 sterol isomerase | Enzyme | Ki | 9.82 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| N0000166793 | NUI |
| D02625 | KEGG_DRUG |
| C0040988 | UMLSCUI |
| CHEBI:135662 | CHEBI |
| CHEMBL15023 | ChEMBL_ID |
| D014272 | MESH_DESCRIPTOR_UI |
| DB13552 | DRUGBANK_ID |
| 5567 | PUBCHEM_CID |
| 1604 | INN_ID |
| R8869Q7R8I | UNII |
| 10804 | RXNORM |
| 004060 | NDDF |
| 387301006 | SNOMEDCT_US |
| 5478006 | SNOMEDCT_US |
| R8869Q7R8I | INXIGHT DRUGS |
Pharmaceutical products:
None