HALOXAZOLAM

Details

Stereochemistry	RACEMIC
Molecular Formula	C17H14BrFN2O2
Molecular Weight	377.208
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

FC1=C(C=CC=C1)C23OCCN2CC(=O)NC4=C3C=C(Br)C=C4

InChI

InChIKey=XDKCGKQHVBOOHC-UHFFFAOYSA-N

InChI=1S/C17H14BrFN2O2/c18-11-5-6-15-13(9-11)17(12-3-1-2-4-14(12)19)21(7-8-23-17)10-16(22)20-15/h1-6,9H,7-8,10H2,(H,20,22)

HIDE SMILES / InChI

Molecular Formula	C17H14BrFN2O2
Molecular Weight	377.208
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: http://www.rad-ar.or.jp/siori/english/kekka.cgi?n=1591

Haloxazolam is a GABA-A receptor agonist indicated for the treatment of anxiety. The drug is approved and marketed in Japan under the name Somelin.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
GABA-A receptor; benzodiazepine site 38 Target ID: CHEMBL2109243 Sources: http://www.rad-ar.or.jp/siori/english/kekka.cgi?n=1591	Agonist 2752

Conditions

Condition	Modality	Targets	Highest Phase	Product
Anxiety 275 Sources: http://www.rad-ar.or.jp/siori/english/kekka.cgi?n=1591 http://www.info.pmda.go.jp/downfiles/ph/GUI/430574_1124005C1032_1_06G.pdf	Primary		Approved 8583	SOMELIN Approved Use Unknown

C_max

Value	Dose	Analyte	Population
48.3 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/530258_1124005C1032_2_003_1F.pdf#page=22	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	FLUBROMAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
58.6 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/530258_1124005C1032_2_003_1F.pdf#page=23	5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	FLUBROMAZEPAM plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
14.3 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/530258_1124005C1032_2_003_1F.pdf#page=23	5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	FLUBROMAZEPAM plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
42 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/530258_1124005C1032_2_003_1F.pdf#page=22	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:		FLUBROMAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
43.2 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/530258_1124005C1032_2_003_1F.pdf#page=23	5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FLUBROMAZEPAM plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
10 mg 1 times / day multiple, oral Studied dose Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/12519461/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/12519461/	Sources: https://pubmed.ncbi.nlm.nih.gov/12519461/

PubMed

Title	Date	PubMed
Long-, intermediate- and short-acting benzodiazepine effects on human sleep EEG spectra.	2003-02	12519461
Solid-phase microextraction and GC-ECD of benzophenones for detection of benzodiazepines in urine.	1999-02-18	10022210
The behavior of 1,4-benzodiazepine drugs in acidic media. V. Kinetics of hydrolysis of flutazolam and haloxazolam in aqueous solution.	1986-01	2870816
[The behavior of 1,4-benzodiazepine drugs in the acidic media. I. Proton and carbon 13 nuclear magnetic resonance spectra of oxazolam, cloxazolam and haloxazolam in the acidic media].	1984-06	6150102
Comparative study on the effects of haloxazolam and estazolam, new sleep inducing drugs, on the alpha- and gamma-motor systems.	1983-10	6139494

Sample Use Guides

In Vivo Use Guide

The drug is usually administered orally at bedtime at dose 5-10mg.

Route of Administration: Oral

In Vitro Use Guide

Unknown

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:37:24 GMT 2025` Edited by `admin` on `Mon Mar 31 18:37:24 GMT 2025`
Record UNII	M448L2V8XP
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

SOMELIN

Preferred Name

English

HALOXAZOLAM

Official Name

English

haloxazolam [INN]

Common Name

English

HALOXAZOLAM [JAN]

Common Name

English

HALOXAZOLAM [MI]

Common Name

English

HALOXAZOLAM [MART.]

Common Name

English

Haloxazolam [WHO-DD]

Common Name

English

10-BROMO-11B-(O-FLUOROPHENYL)-2,3,7,11B-TETRAHYDROOXAZOLO(3,2-D)(1,4)BENZODIAZEPIN-6(5H)-ONE

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1012