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thiethylperazine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2630 | 1420-55-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A dopamine antagonist that is particularly useful in treating the nausea and vomiting associated with anesthesia, mildly emetic cancer chemotherapy agents, radiation therapy, and toxins. This piperazine phenothiazine does not prevent vertigo or motion sickness. (From AMA Drug Evaluations Annual, 1994, p457)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 13 | mg | O |
| 13 | mg | P |
| 13 | mg | R |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.83 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.937 | Moderate | 0.73 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.285 | Moderate | 0.73 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 15.031 | 10^-6 cm/s | Moderate | 0.73 |
| dh-clint | Dog hepatocyte intrinsic clearance | 38.637 | uL/min/10^6 cells | Moderate | 0.73 |
| dppb | Dog plasma protein binding (% unbound) | 1.110 | % | Moderate | 0.73 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 2.650 | % | Moderate | 0.73 |
| herg | hERG pIC50 | 6.023 | pIC50 | Moderate | 0.73 |
| hh-clint | Human hepatocyte intrinsic clearance | 12.942 | uL/min/10^6 cells | Moderate | 0.73 |
| hlm-clint | Human liver microsomal intrinsic clearance | 52.240 | uL/min/mg protein | Moderate | 0.73 |
| hppb | Human plasma protein binding (% unbound) | 0.800 | % | Moderate | 0.73 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,INSR,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK | 54 | |||
| kinase-selectivity-class | AXL,EPHB4,PDK4 | 3 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.914 | Moderate | 0.73 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 185.780 | Moderate | 0.73 | |
| mppb | Mouse plasma protein binding (% unbound) | 1.270 | Moderate | 0.73 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 4.102 | Moderate | 0.73 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 4.960 | % | Moderate | 0.73 |
| rh-clint | Rat hepatocyte intrinsic clearance | 261.818 | uL/min/10^6 cells | Moderate | 0.73 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 6.360 | % | Moderate | 0.73 |
| rppb | Rat plasma protein binding (% unbound) | 1.280 | % | Moderate | 0.73 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 82.414 | uM | Moderate | 0.73 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 18, 1961 | FDA | NOVARTIS |
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 | R06AD03 | RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Phenothiazine derivatives |
| MeSH PA | D000932 | Antiemetics |
| MeSH PA | D005765 | Gastrointestinal Agents |
| MeSH PA | D015259 | Dopamine Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018492 | Dopamine Antagonists |
| CHEBI has role | CHEBI:37930 | phenothiazine antipsychotic drug |
| CHEBI has role | CHEBI:37956 | histamine antagonist |
| CHEBI has role | CHEBI:48279 | serotonergic antagonist |
| CHEBI has role | CHEBI:48561 | dopaminergic antagonist |
| CHEBI has role | CHEBI:48876 | muscarinic antagonist |
| CHEBI has role | CHEBI:50919 | antiemetic |
| CHEBI has role | CHEBI:149553 | anticoronaviral agent |
Related Drugs by ATC class:
R06AD Phenothiazine derivatives 8 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Nausea and vomiting | indication | 16932000 | |
| Vomiting | indication | 422400008 | |
| Nausea | indication | 422587007 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.74 | Basic |
| pKa2 | 4.74 | Basic |
| pKa3 | 3.2 | 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 | 8.70 | WOMBAT-PK | CHEMBL | |||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 7.16 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 6.16 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 7 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 7 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 7 | WOMBAT-PK | |||||
| Alpha-1A adrenergic receptor | GPCR | Ki | 8.70 | WOMBAT-PK | |||||
| D(3) dopamine receptor | GPCR | Ki | 8.70 | WOMBAT-PK | |||||
| Histamine H1 receptor | GPCR | Ki | 7.60 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | WOMBAT-PK | |||||||
| Muscarinic acetylcholine receptor M2 | GPCR | WOMBAT-PK | |||||||
| Muscarinic acetylcholine receptor M3 | GPCR | WOMBAT-PK | |||||||
| Muscarinic acetylcholine receptor M4 | GPCR | WOMBAT-PK | |||||||
| Muscarinic acetylcholine receptor M5 | GPCR | WOMBAT-PK | |||||||
| D(1A) dopamine receptor | GPCR | Ki | 6.30 | WOMBAT-PK | |||||
| FAD-linked sulfhydryl oxidase ALR | Enzyme | AC50 | 5.96 | CHEMBL | |||||
| Pleiotropic ABC efflux transporter of multiple drugs | Transporter | IC50 | 5.64 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019943 | VUID |
| N0000148028 | NUI |
| D02354 | KEGG_DRUG |
| 4019064 | VANDF |
| 4019943 | VANDF |
| C0039865 | UMLSCUI |
| CHEBI:9544 | CHEBI |
| CHEMBL1378 | ChEMBL_ID |
| CHEMBL2359670 | ChEMBL_ID |
| CHEMBL3989478 | ChEMBL_ID |
| D013847 | MESH_DESCRIPTOR_UI |
| DB00372 | DRUGBANK_ID |
| 5440 | PUBCHEM_CID |
| 7306 | IUPHAR_LIGAND_ID |
| 1034 | INN_ID |
| 52239-63-1 | SECONDARY_CAS_RN |
| 1179-69-7 | SECONDARY_CAS_RN |
| 8ETK1WAF6R | UNII |
| 10471 | RXNORM |
| 5567 | MMSL |
| d00857 | MMSL |
| 001491 | NDDF |
| 004595 | NDDF |
| 18321003 | SNOMEDCT_US |
| 36218003 | SNOMEDCT_US |
| 372719002 | SNOMEDCT_US |
| 86659000 | SNOMEDCT_US |
Pharmaceutical products:
None