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buflomedil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| vasodilators | 422 | 55837-25-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.60 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 23.60 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 28.88 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 65 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1.30 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 5.60 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.40 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 3.30 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -0.123 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 2.742 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 9.397 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 4.074 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 76.270 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 83.810 | % | High | 1 |
| herg | hERG pIC50 | 4.555 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.641 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.926 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 73.720 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK1,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 | 49 | |||
| kinase-selectivity-class | AXL,BRAF,DDR1,EIF2AK3,EPHB4,ERBB2,GRK2,MAPK7,MTOR,PDK4,SIK2,TEK,TTK | 13 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 0.542 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.560 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 65.313 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 74.390 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 4.786 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 82.980 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.106 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 37.411 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 91.230 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 75.250 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 922.571 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1976 | 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 | C04AX20 | CARDIOVASCULAR SYSTEM PERIPHERAL VASODILATORS PERIPHERAL VASODILATORS Other peripheral vasodilators |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D014665 | Vasodilator Agents |
Related Drugs by ATC class:
C04AX Other peripheral vasodilators 16 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 | 9.31 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Alpha-2A adrenergic receptor | GPCR | WOMBAT-PK | |||||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 5.89 | CHEMBL | |||||
| 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase | Enzyme | Ki | 7.22 | CHEMBL | |||||
| Alpha-1A adrenergic receptor | GPCR | WOMBAT-PK | |||||||
| Alpha-2C adrenergic receptor | GPCR | WOMBAT-PK | |||||||
| Alpha-1D adrenergic receptor | GPCR | WOMBAT-PK | |||||||
| Alpha-1B adrenergic receptor | GPCR | WOMBAT-PK | |||||||
| Voltage-dependent calcium channel gamma-1 subunit | Ion channel | WOMBAT-PK | |||||||
| C-8 sterol isomerase | Enzyme | Ki | 5.15 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D07176 | KEGG_DRUG |
| 35543-24-9 | SECONDARY_CAS_RN |
| 19836 | RXNORM |
| C0054207 | UMLSCUI |
| CHEBI:94538 | CHEBI |
| CHEMBL188921 | ChEMBL_ID |
| DB13510 | DRUGBANK_ID |
| C010651 | MESH_SUPPLEMENTAL_RECORD_UI |
| 2467 | PUBCHEM_CID |
| 3735 | INN_ID |
| V7I71DQ432 | UNII |
| 703405005 | SNOMEDCT_US |
| 004291 | NDDF |
| 004292 | NDDF |
| V7I71DQ432 | INXIGHT DRUGS |
Pharmaceutical products:
None