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mebhydrolin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1643 | 524-81-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
see also record for mebhydroline, RN: 524-81-2
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.20 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 15.51 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 | 2.998 | Moderate | 0.71 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.475 | Moderate | 0.71 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 28.973 | 10^-6 cm/s | Moderate | 0.71 |
| dh-clint | Dog hepatocyte intrinsic clearance | 79.068 | uL/min/10^6 cells | Moderate | 0.71 |
| dppb | Dog plasma protein binding (% unbound) | 8.130 | % | Moderate | 0.71 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 19.170 | % | Moderate | 0.71 |
| herg | hERG pIC50 | 6.099 | pIC50 | Moderate | 0.71 |
| hh-clint | Human hepatocyte intrinsic clearance | 7.962 | uL/min/10^6 cells | Moderate | 0.71 |
| hlm-clint | Human liver microsomal intrinsic clearance | 25.235 | uL/min/mg protein | Moderate | 0.71 |
| hppb | Human plasma protein binding (% unbound) | 9.240 | % | Moderate | 0.71 |
| kinase-safety-class | ACVR2B,AKT2,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK2,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MET,NTRK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK3,STK33,TEK,TGFBR1,TTK | 33 | |||
| kinase-selectivity-class | AXL | 1 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.441 | Moderate | 0.71 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 153.109 | Moderate | 0.71 | |
| mppb | Mouse plasma protein binding (% unbound) | 9.760 | Moderate | 0.71 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.979 | Moderate | 0.71 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 20.750 | % | Moderate | 0.71 |
| rh-clint | Rat hepatocyte intrinsic clearance | 311.889 | uL/min/10^6 cells | Moderate | 0.71 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 29.950 | % | Moderate | 0.71 |
| rppb | Rat plasma protein binding (% unbound) | 9.110 | % | Moderate | 0.71 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 213.796 | uM | Moderate | 0.71 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1954 | YEAR INTRODUCED |
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 | R06AX15 | RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Other antihistamines for systemic use |
Related Drugs by ATC class:
R06AX Other antihistamines for systemic use 26 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Allergic rhinitis | indication | 61582004 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.31 | 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 | 7.12 | WOMBAT-PK | KEGG DRUG | |||
| Histamine H4 receptor | GPCR | WOMBAT-PK | |||||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 6.75 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 5A | GPCR | Ki | 6.92 | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| D01786 | KEGG_DRUG |
| 6153-33-9 | SECONDARY_CAS_RN |
| CHEBI:135144 | CHEBI |
| CHEMBL1625607 | ChEMBL_ID |
| C025079 | MESH_SUPPLEMENTAL_RECORD_UI |
| C005139 | MESH_SUPPLEMENTAL_RECORD_UI |
| 896 | INN_ID |
| DB13808 | DRUGBANK_ID |
| 9SUK9B7XVY | UNII |
| 22822 | RXNORM |
| 003997 | NDDF |
| 320747007 | SNOMEDCT_US |
| 419632002 | SNOMEDCT_US |
| C0065834 | UMLSCUI |
| 22530 | PUBCHEM_CID |
| 9SUK9B7XVY | INXIGHT DRUGS |
Pharmaceutical products:
None