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diphenylpyraline 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 920 | 147-20-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
an antihistamine used to treat allergic rhinitis, hay fever, and allergic skin disorders, diphenylpyraline blocks the action of endogenous histamine at the histamine H1 receptor
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 10 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 3.81 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,TTK | 47 | |||
| kinase-selectivity-class | AXL,PDK4,SIK2 | 3 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | Moderate | 0.65 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| None | FDA | GLAXOSMITHKLINE |
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 |
|---|---|---|---|---|---|---|
| Neutrophil count decreased | 61.08 | 60.72 | 13 | 49 | 71519 | 90556866 |
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 | R06AA07 | RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Aminoalkyl ethers |
| ATC | R06AA57 | RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Aminoalkyl ethers |
| CHEBI has role | CHEBI:37955 | H<small><sub>1</sub></small>-receptor antagonist |
| CHEBI has role | CHEBI:48873 | cholinergic antagonist |
Related Drugs by ATC class:
R06AA Aminoalkyl ethers 8 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Dermatographic urticaria | indication | 7632005 | DOID:743 |
| Vasomotor rhinitis | indication | 8229003 | DOID:4730 |
| 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 |
| Anaphylaxis Adjunct | indication | ||
| Ocular hypertension | contraindication | 4210003 | DOID:9282 |
| Peptic ulcer | contraindication | 13200003 | DOID:750 |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Chronic idiopathic constipation | contraindication | 82934008 | |
| Bladder outflow obstruction | contraindication | 236645006 | |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Retention of urine | contraindication | 267064002 | |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.56 | 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 | ANTAGONIST | Ki | 8.08 | WOMBAT-PK | CHEMBL | |||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 7.70 | WOMBAT-PK | |||||
| Sodium-dependent dopamine transporter | Transporter | IC50 | 6.38 | WOMBAT-PK | |||||
| Cytochrome P450 2D6 | Enzyme | WOMBAT-PK | |||||||
| Sodium-dependent dopamine transporter | Transporter | IC50 | 6.38 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019727 | VUID |
| N0000147819 | NUI |
| D01172 | KEGG_DRUG |
| 203155 | RXNORM |
| 4018010 | VANDF |
| 4019727 | VANDF |
| C0058389 | UMLSCUI |
| CHEBI:59788 | CHEBI |
| CHEMBL1492 | ChEMBL_ID |
| CHEMBL1564 | ChEMBL_ID |
| DB01146 | DRUGBANK_ID |
| C009871 | MESH_SUPPLEMENTAL_RECORD_UI |
| 3103 | PUBCHEM_CID |
| 7165 | IUPHAR_LIGAND_ID |
| 695 | INN_ID |
| 132-18-3 | SECONDARY_CAS_RN |
| 33361OE3AV | UNII |
| 003403 | NDDF |
| 004800 | NDDF |
| 387476001 | SNOMEDCT_US |
| 712725009 | SNOMEDCT_US |
| 81646007 | SNOMEDCT_US |
| 33361OE3AV | INXIGHT DRUGS |
Pharmaceutical products:
None