alpidem Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
hypnotics/sedatives, zolpidem derivatives 134 82626-01-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • alpidem
  • ananxyl
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 Alpidem was briefly marketed for the treatment of anxiety, but was withdrawn because of liver toxicity.
  • Molecular weight: 404.34
  • Formula: C21H23Cl2N3O
  • CLOGP: 5.58
  • LIPINSKI: 1
  • HAC: 4
  • HDO: 0
  • TPSA: 37.61
  • ALOGS: -5.49
  • ROTB: 7

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Hosey CM, Chan R, Benet LZ

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1991 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
MeSH PA D014151 Anti-Anxiety Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Anxiety disorder indication 197480006 DOID:2030

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 5.34 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
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 Unclassified IC50 4.64 CHEMBL

External reference:

IDSource
I93SC245QZ UNII
D02833 KEGG_DRUG
C0051484 UMLSCUI
CHEBI:135649 CHEBI
CHEMBL54349 ChEMBL_ID
54897 PUBCHEM_CID
5740 INN_ID
C052036 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None