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pecazine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1688 | 60-89-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
major descriptor (66-85); on-line search PHENOTHIAZINES (66-85); Index Medicus search MEPAZINE (66-85); RN given refers to parent cpd
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Hosey CM, Chan R, Benet LZ |
| S (Water solubility) | 0.01 mg/mL | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.870 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.995 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 24.774 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 79.983 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 2.770 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 9.560 | % | High | 1 |
| herg | hERG pIC50 | 5.814 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 9.397 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 19.907 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 3.400 | % | High | 1 |
| kinase-safety-class | ACVR2B,AKT2,AXL,BRAF,CAMK2B,CAMK2D,CDK5,EIF2AK3,ERBB2,GRK2,ITK,MAPK10,MET,NTRK2,PDK2,PDK4,PIM2,PRKDC | 18 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 0.671 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.303 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 181.134 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 4.930 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 6.730 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 13.280 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.266 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 327.341 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 25.220 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 5.730 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 641.210 | 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:
None
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Dermatographic urticaria | indication | 7632005 | DOID:743 |
| Angioedema | indication | 41291007 | DOID:1558 |
| General anesthesia | indication | 50697003 | |
| Allergic rhinitis | indication | 61582004 | |
| Nasal discharge | indication | 64531003 | |
| Nasal congestion | indication | 68235000 | |
| Sneezing | indication | 76067001 | |
| Urticaria | indication | 126485001 | |
| Itching of skin | indication | 418363000 | |
| Allergic conjunctivitis | indication | 473460002 | DOID:11204 |
| Alcoholism | contraindication | 7200002 | |
| Organophosphate poisoning | contraindication | 8260003 | |
| Weight gain finding | contraindication | 8943002 | |
| Neuroleptic malignant syndrome | contraindication | 15244003 | DOID:14464 |
| Senile dementia | contraindication | 15662003 | |
| Chronic disease of respiratory system | contraindication | 17097001 | |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Glaucoma | contraindication | 23986001 | DOID:1686 |
| Orthostatic hypotension | contraindication | 28651003 | |
| Torsades de pointes | contraindication | 31722008 | |
| Parkinsonism | contraindication | 32798002 | |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Chronic heart failure | contraindication | 48447003 | |
| Bradycardia | contraindication | 48867003 | |
| Extrapyramidal disease | contraindication | 76349003 | |
| Hyperglycemia | contraindication | 80394007 | DOID:4195 |
| Epilepsy | contraindication | 84757009 | DOID:1826 |
| Leukopenia | contraindication | 84828003 | DOID:615 |
| Stupor | contraindication | 89458003 | |
| Tardive dyskinesia | contraindication | 102449007 | |
| Prolonged QT interval | contraindication | 111975006 | |
| Acute disease of cardiovascular system | contraindication | 128487001 | |
| Angina pectoris | contraindication | 194828000 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Metabolic syndrome X | contraindication | 237602007 | DOID:14221 |
| Hyperprolactinemia | contraindication | 237662005 | DOID:12700 |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Retention of urine | contraindication | 267064002 | |
| Anemia | contraindication | 271737000 | DOID:2355 |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
| Coma | contraindication | 371632003 | |
| At risk for aspiration | contraindication | 371736008 | |
| Visual impairment | contraindication | 397540003 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Myocardial ischemia | contraindication | 414795007 | DOID:3393 |
| Obesity | contraindication | 414916001 | DOID:9970 |
| Congenital long QT syndrome | contraindication | 442917000 | |
| Carcinoma of female breast | contraindication | 447782002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.07 | Basic |
| pKa2 | 3.55 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Alpha-2A adrenergic receptor | GPCR | Ki | 6.26 | DRUG MATRIX | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 7.12 | DRUG MATRIX | |||||
| Sodium-dependent noradrenaline transporter | Transporter | Ki | 5.73 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 6.96 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 6.49 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 6.59 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 6 | GPCR | Ki | 6.07 | DRUG MATRIX | |||||
| Alpha-2B adrenergic receptor | GPCR | Ki | 6.74 | DRUG MATRIX | |||||
| D(3) dopamine receptor | GPCR | Ki | 6.17 | DRUG MATRIX | |||||
| Histamine H1 receptor | GPCR | Ki | 8.50 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 7.72 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M2 | GPCR | Ki | 6.70 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 7.40 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | Ki | 7.72 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M5 | GPCR | Ki | 7.55 | DRUG MATRIX | |||||
| Alpha-1D adrenergic receptor | GPCR | Ki | 7.24 | DRUG MATRIX | |||||
| FAD-linked sulfhydryl oxidase ALR | Enzyme | AC50 | 7.01 | CHEMBL | |||||
| Mucosa-associated lymphoid tissue lymphoma translocation protein 1 | Enzyme | IC50 | 6.38 | CHEMBL | |||||
| Alpha-1B adrenergic receptor | GPCR | Ki | 7.47 | DRUG MATRIX | |||||
| Membrane-associated progesterone receptor component 1 | Membrane receptor | Ki | 6.41 | DRUG MATRIX | |||||
| Alpha-1A adrenergic receptor | GPCR | IC50 | 6.84 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D02607 | KEGG_DRUG |
| CHEBI:748798 | CHEBI |
| CHEMBL395110 | ChEMBL_ID |
| CHEMBL1712842 | ChEMBL_ID |
| C100190 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9782 | IUPHAR_LIGAND_ID |
| 001484 | NDDF |
| 9663002 | SNOMEDCT_US |
| C0065954 | UMLSCUI |
| 523 | INN_ID |
| 6075 | PUBCHEM_CID |
| PH34873A38 | UNII |
Pharmaceutical products:
None