FLUTOPRAZEPAM

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 Search

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

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.mimaki-family-japan.com/item/detail?item_prefix=TF&item_code=010277&item_branch=002
Curator's Comment: description was created based on several sources, including, http://www.ncbi.nlm.nih.gov/pubmed/6148044

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

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
GABA-A receptor; benzodiazepine site 38 Target ID: CHEMBL2109243 Sources: https://www.mimaki-family-japan.com/item/detail?item_prefix=TF&item_code=010277&item_branch=002	Agonist 2752		13.0 nM [Ki]

Conditions

Condition	Modality	Highest Phase	Product
Anxiety 275 Sources: http://www.ncbi.nlm.nih.gov/pubmed/6148044	Primary	Approved 8583	RESTAS Approved Use It is usually used for the improvement of anxiety, stress and depression; fatigability; and sleep disorder associated with neurosis and psychosomatic disorder (hypertension, gastric and duodenal ulcer, chronic gastritis, irritable bowel syndrome), and psychosomatic symptoms.
Sleep disorder 25 Sources: https://www.mimaki-family-japan.com/item/detail?item_prefix=TF&item_code=010277&item_branch=002	Primary	Approved 8583	RESTAS Approved Use It is usually used for the improvement of anxiety, stress and depression; fatigability; and sleep disorder associated with neurosis and psychosomatic disorder (hypertension, gastric and duodenal ulcer, chronic gastritis, irritable bowel syndrome), and psychosomatic symptoms.
Stress and depression 1 Sources: https://www.mimaki-family-japan.com/item/detail?item_prefix=TF&item_code=010277&item_branch=002	Primary	Approved 8583	RESTAS Approved Use It is usually used for the improvement of anxiety, stress and depression; fatigability; and sleep disorder associated with neurosis and psychosomatic disorder (hypertension, gastric and duodenal ulcer, chronic gastritis, irritable bowel syndrome), and psychosomatic symptoms.

C_max

Value	Dose	Analyte	Population
2.7 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2633923/	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	FLUTOPRAZEPAM serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
24.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2633923/	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	NORFLURAZEPAM serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
38.7 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/5/580591_1124027F1035_5_006_1F.pdf#page=19	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	NORFLURAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
93.3 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/5/580591_1124027F1035_5_006_1F.pdf#page=19	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	NORFLURAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
163.3 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/5/580591_1124027F1035_5_006_1F.pdf#page=19	8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:	NORFLURAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
273 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/5/580591_1124027F1035_5_006_1F.pdf#page=19	12 mg single, oral dose: 12 mg route of administration: Oral experiment type: SINGLE co-administered:	NORFLURAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
370.3 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/5/580591_1124027F1035_5_006_1F.pdf#page=19	16 mg single, oral dose: 16 mg route of administration: Oral experiment type: SINGLE co-administered:	NORFLURAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED

AUC

Value	Dose	Co-administered	Analyte	Population
2.34 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2633923/	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:		NORFLURAZEPAM serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
87.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2633923/	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	NORFLURAZEPAM serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
186.7 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/5/580591_1124027F1035_5_006_1F.pdf#page=19	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	NORFLURAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
132.9 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/5/580591_1124027F1035_5_006_1F.pdf#page=19	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	NORFLURAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
215.5 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/5/580591_1124027F1035_5_006_1F.pdf#page=19	8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:	NORFLURAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
134.2 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/5/580591_1124027F1035_5_006_1F.pdf#page=19	12 mg single, oral dose: 12 mg route of administration: Oral experiment type: SINGLE co-administered:	NORFLURAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
243.6 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/5/580591_1124027F1035_5_006_1F.pdf#page=19	16 mg single, oral dose: 16 mg route of administration: Oral experiment type: SINGLE co-administered:	NORFLURAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED

F_unbound

Value	Dose	Co-administered	Analyte	Population
1.4% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9158878/			NORFLURAZEPAM plasma	Homo sapiens
5% EXPERIMENT https://www.jstage.jst.go.jp/article/jsdt1994/29/10/29_10_1393/_article/-char/en			FLUTOPRAZEPAM plasma	Homo sapiens

Doses

Dose	Population	Adverse events
2 mg single, oral Studied dose Dose: 2 mg Route: oral Route: single Dose: 2 mg Sources: https://pubmed.ncbi.nlm.nih.gov/2633923	healthy Health Status: healthy Sex: M Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/2633923	Sources: https://pubmed.ncbi.nlm.nih.gov/2633923

PubMed

Title	Date	PubMed
Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method.	2010-12	21818443

Patents

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 Created by `admin` on `Mon Mar 31 18:08:27 GMT 2025` Edited by `admin` on `Mon Mar 31 18:08:27 GMT 2025`
Record UNII	2GHY1101MM
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

FLUTOPRAZEPAM

Official Name

English

RESTAS

Preferred Name

English

FLUTOPRAZEPAM [MART.]

Common Name

English

7-CHLORO-1-(CYCLOPROPYLMETHYL)-5-(O-FLUOROPHENYL)-1,3-DIHYDRO-2H-1,4-BENZODIAZEPIN-2-ONE

Common Name

English

FLUTOPRAZEPAM [JAN]

Common Name

English

FLUTOPRAZEPAM [MI]

Common Name

English

flutoprazepam [INN]

Common Name

English

Flutoprazepam [WHO-DD]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1012