New Release: Alpha testing version has been released.

Etifoxine

N05B - Anxiolytics ATC N05BX03 Small molecule Natural product

JFDA label: Stresam 50mg

Mechanism of Action

Antagonist of GABA-A receptor; anion channel — GABA-A receptor; anion channel antagonist

TargetActionGene / class
GABA-A receptor; anion channel efficacy ANTAGONIST

Indications

Off-label

  • Anxiety

Chemistry & Properties

2D structure
FormulaC17H17ClN2O
Molecular weight300.79 g/mol
IUPAC name6-chloro-N-ethyl-4-methyl-4-phenyl-1H-3,1-benzoxazin-2-imine
CAS21715-46-8
PubChem CID135413553
InChIKeyIBYCYJFUEJQSMK-UHFFFAOYSA-N
logP4.23 (XLogP 4.1)
Polar surface area33.62 Ų
H-bond acceptors / donors3 / 1
Drug-likeness (QED)0.90
Lipinski violations0
SMILESCCNC1=Nc2ccc(Cl)cc2C(C)(c2ccccc2)O1

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrantYes

Enzyme interactions

EnzymeRoleDetail
CYP1A2Inhibitor
CYP2B6Inhibitor
CYP2C19Inhibitor
CYP2C19Substrate
CYP2C8Inhibitor
CYP2C9Inhibitor
CYP2D6Inhibitor
CYP3A4Inhibitor
CYP3A4Substrate

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Registered Products (1)

BrandForm / strengthPackAgentCitizen (JOD)
Stresam Tablet 50 mg 60 tab THE ARAB DRUG STORE P.S.C 4.230