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moracizine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| diphenylmethyl piperazine derivatives | 1842 | 31883-05-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An antiarrhythmia agent used primarily for ventricular rhythm disturbances.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.75 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 35.09 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 34 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.063 | Moderate | 0.75 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.964 | Moderate | 0.75 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 53.703 | 10^-6 cm/s | Moderate | 0.75 |
| dh-clint | Dog hepatocyte intrinsic clearance | 41.115 | uL/min/10^6 cells | Moderate | 0.75 |
| dppb | Dog plasma protein binding (% unbound) | 8.450 | % | Moderate | 0.75 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 18.430 | % | Moderate | 0.75 |
| herg | hERG pIC50 | 4.884 | pIC50 | Moderate | 0.75 |
| hh-clint | Human hepatocyte intrinsic clearance | 30.200 | uL/min/10^6 cells | Moderate | 0.75 |
| hlm-clint | Human liver microsomal intrinsic clearance | 171.396 | uL/min/mg protein | Moderate | 0.75 |
| hppb | Human plasma protein binding (% unbound) | 6.210 | % | Moderate | 0.75 |
| kinase-safety-class | ACVR2B,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK2,JAK3,MAP3K1,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK | 51 | |||
| kinase-selectivity-class | AXL,DDR1,GRK2,MAPK7,PDK4,STK33,TEK,TTK | 8 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.588 | Moderate | 0.75 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 150.661 | Moderate | 0.75 | |
| mppb | Mouse plasma protein binding (% unbound) | 8.770 | Moderate | 0.75 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 8.650 | Moderate | 0.75 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 15.910 | % | Moderate | 0.75 |
| rh-clint | Rat hepatocyte intrinsic clearance | 215.774 | uL/min/10^6 cells | Moderate | 0.75 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 59.160 | % | Moderate | 0.75 |
| rppb | Rat plasma protein binding (% unbound) | 9.400 | % | Moderate | 0.75 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 52 | uM | Moderate | 0.75 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 19, 1990 | FDA |
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 | C01BG01 | CARDIOVASCULAR SYSTEM CARDIAC THERAPY ANTIARRHYTHMICS, CLASS I AND III Other antiarrhythmics, class I and III |
| FDA EPC | N0000175426 | Antiarrhythmic |
| MeSH PA | D000889 | Anti-Arrhythmia Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D026941 | Sodium Channel Blockers |
| MeSH PA | D049990 | Membrane Transport Modulators |
| MeSH PA | D061567 | Voltage-Gated Sodium Channel Blockers |
| CHEBI has role | CHEBI:38070 | anti-arrhythmia drug |
Related Drugs by ATC class:
C01BG Other antiarrhythmics, class I and III 2 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Ventricular arrhythmia | indication | 44103008 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 11.75 | acidic |
| pKa2 | 6.21 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Sodium channel protein type 5 subunit alpha | Ion channel | BLOCKER | WOMBAT-PK | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019551 | VUID |
| N0000179669 | NUI |
| D02087 | KEGG_DRUG |
| 29560-58-5 | SECONDARY_CAS_RN |
| 4019551 | VANDF |
| 4019845 | VANDF |
| C0079856 | UMLSCUI |
| CHEBI:6997 | CHEBI |
| CHEMBL1075 | ChEMBL_ID |
| CHEMBL1200334 | ChEMBL_ID |
| DB00680 | DRUGBANK_ID |
| 34633 | PUBCHEM_CID |
| 7244 | IUPHAR_LIGAND_ID |
| 151721 | RXNORM |
| 1620 | MMSL |
| 5135 | MMSL |
| d00307 | MMSL |
| 003553 | NDDF |
| 004488 | NDDF |
| 108489008 | SNOMEDCT_US |
| 350598002 | SNOMEDCT_US |
| 373726009 | SNOMEDCT_US |
| D016293 | MESH_DESCRIPTOR_UI |
| 2998 | INN_ID |
| 71OK3Z1ESP | UNII |
Pharmaceutical products:
None