Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00574)
Name
Quazepam
Synonyms    Click to Show/Hide the Synonyms of This API
quazepam; Prosedar; Quazium; Dormalin; Oniria; Selepam; 36735-22-5; Sch 16134; Quazepamum [INN-Latin]; Sch-16134; UNII-JF8V0828ZI; 7-chloro-5-(2-fluorophenyl)-1-(2,2,2-trifluoroethyl)-3H-1,4-benzodiazepine-2-thione; 7-Chloro-5-(o-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-2H-1,4-benzodiazepine-2-thione; CHEBI:8694; JF8V0828ZI; Quazepamum; Quazapam; NSC-309702; 2H-1,4-Benzodiazepine-2-thione, 7-chloro-5-(2-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-; Cetrane; Doral [Sedative]; 7-chloro-5-(2-fluorophenyl)-1-(2,2,2-trifluoroethyl)-2,3-dihydro-1H-1,4-benzodiazepine-2-thione; Doral (TN); EINECS 253-179-4; NSC 309702; Quazepam (JAN/USP/INN); Sch-161; BRN 0901084; Quazepam civ; DEA No. 2881; Quazepam [USAN:USP:INN:BAN]; Quazepam civ(200 mg); SCHEMBL29504; 5-24-04-00356 (Beilstein Handbook Reference); GTPL7288; CHEMBL1200472; DTXSID60190193; ZINC538266; NSC309702; DB01589; C07336; D00457; 735Q225; Q3927403; 2H-1, 7-chloro-5-(2-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-; 7-Chloro-5-(o-fluorophenyl)-1,2,2-trifluoroethyl)-2H-1,4-benzodiazepine-2-thione
Clinical Status
Approved
Disease Indication Insomnia ICD-11: 7A00 [1]
PubChem CID
4999
Formula
C17H11ClF4N2S
Canonical SMILES
C1C(=S)N(C2=C(C=C(C=C2)Cl)C(=N1)C3=CC=CC=C3F)CC(F)(F)F
InChI
1S/C17H11ClF4N2S/c18-10-5-6-14-12(7-10)16(11-3-1-2-4-13(11)19)23-8-15(25)24(14)9-17(20,21)22/h1-7H,8-9H2
InChIKey
IKMPWMZBZSAONZ-UHFFFAOYSA-N
   Click to Show/Hide the Molecular Data (Structure/Property) of This API
Structure
<iframe style="width: 300px; height: 300px;" frameborder="0" src="https://embed.molview.org/v1/?mode=balls&cid=4999"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 386.8 Topological Polar Surface Area 47.7
XlogP 4 Complexity 539
Heavy Atom Count 25 Rotatable Bond Count 2
Hydrogen Bond Donor Count 0 Hydrogen Bond Acceptor Count 6
Full List of Drug Formulations (DFMs) Containing This API
          Quazepam 15 mg tablet Click to Show/Hide the Full List of Formulation(s):          1 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose; Sodium lauryl sulfate; Fd&c yellow no. 6; Magnesium stearate; Silicon dioxide; Powdered cellulose; Starch, corn
                   Dosage Form Oral Tablet
                   Company Bryant Ranch Prepack; Galt Pharmaceuticals; Thompson Medical Solutions; Unit Dose Services
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
References
1 FDA label for approved quazepam from the official website of the U.S. Food and Drug Administration.
2 Bacterial metabolism rescues the inhibition of intestinal drug absorption by food and drug additives. Proc Natl Acad Sci U S A. 2020 Jul 7;117(27):16009-16018.
3 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.

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