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bromperidol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antipsychotics, haloperidol derivatives | 407 | 10457-90-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
bromine-substituted for chlorine in haloperidol; RN given refers to unlabeled parent cpd; structure
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 10 | mg | O |
| 10 | mg | P |
| 3.30 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.09 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0.50 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 1.98 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 50 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.034 | High | 0.83 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.698 | High | 0.83 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 29.444 | 10^-6 cm/s | High | 0.83 |
| dh-clint | Dog hepatocyte intrinsic clearance | 15.959 | uL/min/10^6 cells | High | 0.83 |
| dppb | Dog plasma protein binding (% unbound) | 11.650 | % | High | 0.83 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 34.160 | % | High | 0.83 |
| herg | hERG pIC50 | 6.782 | pIC50 | High | 0.83 |
| hh-clint | Human hepatocyte intrinsic clearance | 2.360 | uL/min/10^6 cells | High | 0.83 |
| hlm-clint | Human liver microsomal intrinsic clearance | 14.421 | uL/min/mg protein | High | 0.83 |
| hppb | Human plasma protein binding (% unbound) | 11.230 | % | High | 0.83 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,ALK,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK1,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK | 52 | |||
| kinase-selectivity-class | AKT2,AKT3,AXL,EIF2AK3,GRK2,PDK4,PRKCD,SIK2 | 8 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 0.389 | High | 0.83 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.598 | High | 0.83 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 23.442 | High | 0.83 | |
| mppb | Mouse plasma protein binding (% unbound) | 12.250 | High | 0.83 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.820 | High | 0.83 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | High | 0.83 | |
| rat-kpuu-brain | Rat brain Kpuu | 0.068 | % | High | 0.83 |
| pppb | Pig plasma protein binding (% unbound) | 23.440 | % | High | 0.83 |
| rh-clint | Rat hepatocyte intrinsic clearance | 53.456 | uL/min/10^6 cells | High | 0.83 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 26.680 | % | High | 0.83 |
| rppb | Rat plasma protein binding (% unbound) | 9.960 | % | High | 0.83 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 28.510 | uM | High | 0.83 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1973 | YEAR INTRODUCED |
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 | N05AD06 | NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Butyrophenone derivatives |
| 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 |
| CHEBI has role | CHEBI:35469 | antidepressant |
| CHEBI has role | CHEBI:35474 | anxiolytic drug |
| 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(2) dopamine receptor | GPCR | ANTAGONIST | Ki | 8.43 | WOMBAT-PK | KEGG DRUG | |||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | EC50 | 9.02 | WOMBAT-PK | |||||
| Alpha-1A adrenergic receptor | GPCR | Ki | 7.10 | WOMBAT-PK | |||||
| D(3) dopamine receptor | GPCR | Ki | 7.50 | WOMBAT-PK | |||||
| Histamine H1 receptor | GPCR | Ki | 6.16 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 5.12 | PDSP | |||||
| Muscarinic acetylcholine receptor M2 | GPCR | Ki | 5.75 | PDSP | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 5.15 | PDSP | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | Ki | 5.77 | PDSP | |||||
| Muscarinic acetylcholine receptor M5 | GPCR | Ki | 5.32 | PDSP | |||||
| D(1A) dopamine receptor | GPCR | Ki | 7 | WOMBAT-PK | |||||
| D(4) dopamine receptor | GPCR | Ki | 7.80 | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| D01101 | KEGG_DRUG |
| 19777 | RXNORM |
| C1369894 | UMLSCUI |
| CHEBI:31305 | CHEBI |
| CHEMBL28218 | ChEMBL_ID |
| DB12401 | DRUGBANK_ID |
| C006820 | MESH_SUPPLEMENTAL_RECORD_UI |
| 2448 | PUBCHEM_CID |
| 3737 | INN_ID |
| LYH6F7I22E | UNII |
| 725571009 | SNOMEDCT_US |
| 006754 | NDDF |
| LYH6F7I22E | INXIGHT DRUGS |
Pharmaceutical products:
None