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ifenprodil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| vasodilators | 1419 | 23210-56-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
NMDA receptor antagonist; RN given refers to parent cpd without isomeric designation; structure
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 18.99 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 64.57 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 4.32 hours | Lombardo F, Berellini G, Obach RS |
| BA (Bioavailability) | 5 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.840 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.982 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 14.859 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 40.365 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 24.110 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 47.640 | % | High | 1 |
| herg | hERG pIC50 | 5.592 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 34.514 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 82.794 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 31.820 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PIK3CB,PIM2,PRKDC,TEK,TGFBR1 | 26 | |||
| kinase-selectivity-class | ACVR2B,AXL,CAMK2D,CDK4,CDK9,EIF2AK3,EPHB4,GRK2,MAP2K6,SIK2,TEK | 11 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 3.083 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.803 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 238.781 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 38.300 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 3.631 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 59.390 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.103 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 261.216 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 70.050 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 40.230 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 895.365 | uM | High | 1 |
Approvals:
None
FDA Adverse Event Reporting System (Female)
None
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 |
|---|---|---|---|---|---|---|
| Inappropriate antidiuretic hormone secretion | 65.93 | 52.76 | 14 | 113 | 16527 | 42604681 |
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 |
|---|---|---|---|---|---|---|
| Inappropriate antidiuretic hormone secretion | 58.19 | 53.40 | 14 | 258 | 33837 | 110555190 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C04AX28 | CARDIOVASCULAR SYSTEM PERIPHERAL VASODILATORS PERIPHERAL VASODILATORS Other peripheral vasodilators |
| MeSH PA | D000317 | Adrenergic alpha-Antagonists |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D014665 | Vasodilator Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018674 | Adrenergic Antagonists |
| MeSH PA | D018691 | Excitatory Amino Acid Antagonists |
| CHEBI has role | CHEBI:35469 | antidepressant |
| CHEBI has role | CHEBI:22587 | antiviral agent |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
| CHEBI has role | CHEBI:35705 | immunosuppressive agent |
| CHEBI has role | CHEBI:233423 | antifibrotic agent |
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 | 10.27 | acidic |
| pKa2 | 9.1 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Glutamate receptor ionotropic, NMDA 2A | Ion channel | IC50 | 4.40 | CHEMBL | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | IC50 | 8.41 | CHEMBL | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 7 | CHEMBL | |||||
| Histamine H1 receptor | GPCR | IC50 | 6 | CHEMBL | |||||
| Glutamate receptor ionotropic, NMDA 2B | Ion channel | IC50 | 7.70 | CHEMBL | |||||
| Glutamate receptor ionotropic, NMDA 2C | Ion channel | IC50 | 4.54 | CHEMBL | |||||
| Glutamate receptor ionotropic, NMDA 2D | Ion channel | IC50 | 4.12 | CHEMBL | |||||
| Glutamate NMDA receptor; GRIN1/GRIN2B | Ion channel | Ki | 8 | CHEMBL | |||||
| Glutamate receptor ionotropic, NMDA 1 | Ion channel | IC50 | 7.14 | CHEMBL | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 8.70 | CHEMBL | |||||
| Alpha-2A adrenergic receptor | GPCR | IC50 | 6.96 | CHEMBL | |||||
| Translocator protein | Membrane receptor | IC50 | 9.14 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | IC50 | 6.62 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | IC50 | 6.21 | CHEMBL | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane other | Ki | 8.99 | CHEMBL | |||||
| Adrenergic receptor alpha-1 | GPCR | IC50 | 7 | CHEMBL | |||||
| Glutamate [NMDA] receptor subunit epsilon 2 | Ion channel | Ki | 7.96 | CHEMBL | |||||
| 3-beta-hydroxysteroid-delta(8),delta(7)-isomerase | Enzyme | Ki | 8.57 | CHEMBL | |||||
| Sigma intracellular receptor 2 | Membrane receptor | Ki | 7.01 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D01445 | KEGG_DRUG |
| C0063340 | UMLSCUI |
| CHEBI:748305 | CHEBI |
| QEL | PDB_CHEM_ID |
| CHEMBL305187 | ChEMBL_ID |
| DB08954 | DRUGBANK_ID |
| CHEMBL1886888 | ChEMBL_ID |
| C010739 | MESH_SUPPLEMENTAL_RECORD_UI |
| 3689 | PUBCHEM_CID |
| 5472 | IUPHAR_LIGAND_ID |
| 3236 | INN_ID |
| 23210-58-4 | SECONDARY_CAS_RN |
| R8OE3P6O5S | UNII |
| 27403 | RXNORM |
| 005790 | NDDF |
| 005791 | NDDF |
| 16291000122106 | SNOMEDCT_US |
| R8OE3P6O5S | INXIGHT DRUGS |
Pharmaceutical products:
None