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alpidem 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| hypnotics/sedatives, zolpidem derivatives | 134 | 82626-01-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Alpidem shows anxiolytic and anticonvulsant properties which appear to be elicited both with a direct mechanism through the interaction with central benzodiazepine receptor (CBR) and with an indirect mechanism by the interaction with peripheral benzodiazepine receptor (PBR) as well as the stimulation of pregnenolone formation. Alpidem was briefly marketed for the treatment of anxiety, but was withdrawn because of liver toxicity.
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
| S (Water solubility) | 0.02 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 | 4.383 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.416 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 53.703 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 37.844 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 1.090 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 1.760 | % | High | 1 |
| herg | hERG pIC50 | 5.321 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 43.451 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 275.423 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.800 | % | High | 1 |
| kinase-safety-class | ACVR2B,ALK,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K1,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MARK4,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CG,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TTK | 43 | |||
| kinase-selectivity-class | ACVR2B,PDK4 | 2 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.484 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 137.721 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.930 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.592 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 1.630 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 184.502 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 15.010 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.980 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 40.644 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1991 | 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 |
|---|---|---|
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D011619 | Psychotropic Drugs |
| MeSH PA | D014149 | Tranquilizing Agents |
| MeSH PA | D014151 | Anti-Anxiety Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Anxiety disorder | indication | 197480006 | DOID:2030 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 5.34 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Gamma-aminobutyric acid receptor subunit alpha-1 | Ion channel | PARTIAL AGONIST | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||||
| Translocator protein | Transporter | Ki | 9.30 | CHEMBL | |||||
| Bile salt export pump | Transporter | IC50 | 5.04 | CHEMBL | |||||
| Translocator protein | Membrane receptor | Ki | 9.30 | CHEMBL | |||||
| GABA-A receptor; anion channel | Ion channel | IC50 | 7.59 | CHEMBL | |||||
| Bile salt export pump | Transporter | IC50 | 4.64 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D02833 | KEGG_DRUG |
| C0051484 | UMLSCUI |
| CHEBI:135649 | CHEBI |
| CHEMBL54349 | ChEMBL_ID |
| C052036 | MESH_SUPPLEMENTAL_RECORD_UI |
| 54897 | PUBCHEM_CID |
| 5740 | INN_ID |
| I93SC245QZ | UNII |
Pharmaceutical products:
None