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Details

Stereochemistry ACHIRAL
Molecular Formula C19H16ClFN2O
Molecular Weight 342.795
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of FLUTOPRAZEPAM

SMILES

FC1=CC=CC=C1C2=NCC(=O)N(CC3CC3)C4=CC=C(Cl)C=C24

InChI

InChIKey=OFVXPDXXVSGEPX-UHFFFAOYSA-N
InChI=1S/C19H16ClFN2O/c20-13-7-8-17-15(9-13)19(14-3-1-2-4-16(14)21)22-10-18(24)23(17)11-12-5-6-12/h1-4,7-9,12H,5-6,10-11H2

HIDE SMILES / InChI
Molecular Formula C19H16ClFN2O
Molecular Weight 342.795
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

Flutoprazepam is a benzodiazepine derivative that reduce anxiety, stress, depression, fatigability and sleep disorders in patients with neurosis and psychosomatic disorders by binding to GABA-A receptor and modulating its activity.

CNS Activity

CNS Active
4,002

Originator

Kanebo
5

Approval Year

Unknown
149,124

Targets

Primary TargetPharmacologyConditionPotency
GABA-A receptor; benzodiazepine site
38
Agonist
2,752
 13.0 nM [Ki]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Anxiety
275
 Primary
Approved
8,583
RESTAS
Sleep disorder
25
 Primary
Approved
8,583
RESTAS
Stress and depression
1
 Primary
Approved
8,583
RESTAS

Cmax

ValueDoseCo-administeredAnalytePopulation
2.7 ng/mL
2 mg single, oral
 FLUTOPRAZEPAM serum
Homo sapiens
24.9 ng/mL
2 mg single, oral
 NORFLURAZEPAM serum
Homo sapiens
38.7 ng/mL
2 mg single, oral
 NORFLURAZEPAM plasma
Homo sapiens
93.3 μg/mL
4 mg single, oral
 NORFLURAZEPAM plasma
Homo sapiens
163.3 ng/mL
8 mg single, oral
 NORFLURAZEPAM plasma
Homo sapiens
273 ng/mL
12 mg single, oral
 NORFLURAZEPAM plasma
Homo sapiens
370.3 ng/mL
16 mg single, oral
 NORFLURAZEPAM plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
2.34 μg × h/mL
2 mg single, oral
 NORFLURAZEPAM serum
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
87.2 h
2 mg single, oral
 NORFLURAZEPAM serum
Homo sapiens
186.7 h
2 mg single, oral
 NORFLURAZEPAM plasma
Homo sapiens
132.9 h
4 mg single, oral
 NORFLURAZEPAM plasma
Homo sapiens
215.5 h
8 mg single, oral
 NORFLURAZEPAM plasma
Homo sapiens
134.2 h
12 mg single, oral
 NORFLURAZEPAM plasma
Homo sapiens
243.6 h
16 mg single, oral
 NORFLURAZEPAM plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
1.4%
NORFLURAZEPAM plasma
Homo sapiens
5%
FLUTOPRAZEPAM plasma
Homo sapiens

Doses

PubMed

Patents

US3632574
1

Sample Use Guides

In Vivo Use Guide
For adults, take 1 to 2 tablets (2 to 4 mg of the active ingredient) in 1 to 2 divided doses daily.
Route of Administration: Oral
In Vitro Use Guide
Unknown
Substance Class Chemical
Record UNII
2GHY1101MM
Record Status Validated (UNII)
Record Version
NIH
NCATS
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