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zotepine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| tricyclic compounds | 2875 | 26615-21-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.20 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Hosey CM, Chan R, Benet LZ |
| BA (Bioavailability) | 10 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| 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,GSK3B,ITK,JAK1,JAK2,JAK3,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK | 55 | |||
| kinase-selectivity-class | AXL,BRAF,PDK4,TTK | 4 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
None
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Neuroleptic malignant syndrome | 66.91 | 59.43 | 15 | 377 | 15081 | 90612974 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Colitis ischaemic | 58.06 | 54.54 | 13 | 319 | 7213 | 42613790 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Neuroleptic malignant syndrome | 92.69 | 46.29 | 25 | 727 | 34034 | 110554513 |
| Psychiatric symptom | 56.53 | 46.29 | 13 | 739 | 9200 | 110579347 |
| Delusion | 48.76 | 46.29 | 14 | 738 | 23741 | 110564806 |
| Colitis ischaemic | 48.06 | 46.29 | 13 | 739 | 17737 | 110570810 |
| Colectomy total | 46.39 | 46.29 | 7 | 745 | 497 | 110588050 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N05AX11 | NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Other antipsychotics |
| 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:48278 | serotonergic drug |
| CHEBI has role | CHEBI:48539 | α-adrenergic drug |
| CHEBI has role | CHEBI:65191 | second generation antipsychotic |
Related Drugs by ATC class:
N05AX Other antipsychotics 11 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 | 8.25 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Histamine H1 receptor | GPCR | Ki | 9.21 | CHEMBL | |||||
| Histamine H2 receptor | GPCR | Ki | 6.30 | PDSP | |||||
| Histamine H4 receptor | GPCR | Ki | 5.70 | PDSP | |||||
| Beta-1 adrenergic receptor | GPCR | Ki | 5.39 | PDSP | |||||
| Beta-2 adrenergic receptor | GPCR | Ki | 5.64 | PDSP | |||||
| D(1A) dopamine receptor | GPCR | Ki | 7.54 | CHEMBL | |||||
| D(2) dopamine receptor | GPCR | Ki | 7.96 | CHEMBL | |||||
| Alpha-2A adrenergic receptor | GPCR | Ki | 6.69 | PDSP | |||||
| Sodium-dependent serotonin transporter | Transporter | Ki | 6.82 | PDSP | |||||
| Sodium-dependent noradrenaline transporter | Transporter | INHIBITOR | IC50 | 7.15 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 6.48 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 9.04 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 8.54 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 6 | GPCR | ANTAGONIST | Ki | 8.30 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 7 | GPCR | ANTAGONIST | Ki | 8.40 | IUPHAR | ||||
| Alpha-1A adrenergic receptor | GPCR | Ki | 8.16 | PDSP | |||||
| Alpha-2B adrenergic receptor | GPCR | Ki | 8.27 | PDSP | |||||
| D(3) dopamine receptor | GPCR | Ki | 8.19 | CHEMBL | |||||
| D(1B) dopamine receptor | GPCR | Ki | 6.61 | PDSP | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 7.75 | PDSP | |||||
| Muscarinic acetylcholine receptor M2 | GPCR | Ki | 6.85 | PDSP | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 7.14 | PDSP | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | Ki | 6.26 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M5 | GPCR | Ki | 6.59 | PDSP | |||||
| 5-hydroxytryptamine receptor 1B | GPCR | ANTAGONIST | Ki | 7.20 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 1D | GPCR | ANTAGONIST | Ki | 9.30 | IUPHAR | ||||
| Alpha-2C adrenergic receptor | GPCR | Ki | 7.02 | PDSP | |||||
| Sodium-dependent dopamine transporter | Transporter | Ki | 5.44 | PDSP | |||||
| D(4) dopamine receptor | GPCR | Ki | 7.41 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 3A | Ion channel | Ki | 6.33 | PDSP | |||||
| Alpha-1B adrenergic receptor | GPCR | Ki | 8.30 | PDSP | |||||
| 5-hydroxytryptamine receptor 5A | GPCR | Ki | 7.54 | PDSP | |||||
| 5-hydroxytryptamine receptor 1E | GPCR | ANTAGONIST | Ki | 6.50 | IUPHAR | ||||
| Histone deacetylase 6 | Enzyme | IC50 | 6.22 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 7 | GPCR | ANTAGONIST | Ki | 8.80 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 6 | GPCR | ANTAGONIST | Ki | 8.90 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| D01321 | KEGG_DRUG |
| C0078849 | UMLSCUI |
| CHEBI:32316 | CHEBI |
| ZOT | PDB_CHEM_ID |
| CHEMBL285802 | ChEMBL_ID |
| DB09225 | DRUGBANK_ID |
| C022172 | MESH_SUPPLEMENTAL_RECORD_UI |
| 5736 | PUBCHEM_CID |
| 103 | IUPHAR_LIGAND_ID |
| 4112 | INN_ID |
| U29O83JAZW | UNII |
| 40003 | RXNORM |
| 007029 | NDDF |
| 321641006 | SNOMEDCT_US |
| 395930007 | SNOMEDCT_US |
| U29O83JAZW | INXIGHT DRUGS |
Pharmaceutical products:
None