Details
Stereochemistry | ACHIRAL |
Molecular Formula | C15H10BrClN4S |
Molecular Weight | 393.689 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=NN=C2CN=C(C3=C(SC(Br)=C3)N12)C4=C(Cl)C=CC=C4
InChI
InChIKey=UMSGKTJDUHERQW-UHFFFAOYSA-N
InChI=1S/C15H10BrClN4S/c1-8-19-20-13-7-18-14(9-4-2-3-5-11(9)17)10-6-12(16)22-15(10)21(8)13/h2-6H,7H2,1H3
Molecular Formula | C15H10BrClN4S |
Molecular Weight | 393.689 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/3281819Curator's Comment: description was created based on several sources, including
http://www.rad-ar.or.jp/siori/english/print.cgi?n=52
Sources: https://www.ncbi.nlm.nih.gov/pubmed/3281819
Curator's Comment: description was created based on several sources, including
http://www.rad-ar.or.jp/siori/english/print.cgi?n=52
Brotizolam (marketed under brand name Lendormin) is a sedative-hypnotic thienotriazolodiazepine drug which is a benzodiazepine analog. It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties, and is considered to be similar in effect to short-acting benzodiazepines such as triazolam. It is used in the short-term treatment of severe or debilitating insomnia and in a dose of 0.25 mg can be used as a premedication prior to surgery, this dose was found to be comparable in efficacy to 2 mg flunitrazepam as a premedicant prior to surgery. The drug was developed by a team led by T Nishiyama while working for Takeda Chemical Industries in 1976 in Japan. Brotizolam is not approved for sale in the UK, United States or Canada. It is approved for sale in the Netherlands, Germany, Spain, Belgium, Luxembourg, Austria, Portugal, Israel, Italy, Taiwan and Japan. Insomnia. Brotizolam is prescribed for the short-term treatment, 2–4 weeks only of severe or debilitating insomnia. Insomnia can be described as a difficulty falling asleep, frequent awakening, early awakenings or a combination of each. Brotizolam inhibits the hypothalamus and cerebral limbic system controlling emotion through GABA, a typical inhibitory transmitter of central nervous system. As a result, unnecessary stimulation from the autonomic nervous system and other sites is blocked, demonstrating central nervous action including hypnosis, sedation and anti-anxiety
CNS Activity
Sources: http://www.ncbi.nlm.nih.gov/pubmed/6151995
Curator's Comment: CNS depressant
Known to be CNS depressant in mice, rats and rabbits. Human data not available
Originator
Sources: https://www.google.com/patents/US4017620
Curator's Comment: # by a team led by T Nishiyama while working for Takeda Chemical Industries in 1976 in Japan
Approval Year
PubMed
Title | Date | PubMed |
---|---|---|
[Actigraphic assessment of the effects of hypnotics on the night before surgery in relation with the severity of surgery]. | 2005 Nov |
|
Paradoxical reactions to hypnotic agents in adolescents with free-running disorder. | 2009 Jun |
|
Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method. | 2010 Dec |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: http://www.rad-ar.or.jp/siori/english/print.cgi?n=52
for adults: one tablet (0.25mg of brotizolam) is orally administered once daily at bedtime
Route of Administration:
Oral
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/6835488
Using slices of the olfactory tubercle, nucleus accumbens and caudate nucleus, the effects of brotizolam on dopaminergic nerve terminals were examined in vitro. Basal release of dopamine was not affected by brotizolam in concentrations up to 10(-6) M; however, K+-stimulated release of dopamine was significantly reduced by brotizolam at 10(-7) M or above. The reduction of K+-stimulated release of dopamine was antagonized by bicuculline, added in the superfusion medium.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:18:45 GMT 2023
by
admin
on
Fri Dec 15 15:18:45 GMT 2023
|
Record UNII |
5XZM1R3DKF
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Brand Name | English | ||
|
Code | English | ||
|
Code | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Code | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
WHO-ATC |
N05CD09
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
||
|
NCI_THESAURUS |
C1012
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
||
|
WHO-VATC |
QN05CD09
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
C87057
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
PRIMARY | |||
|
4549
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
PRIMARY | |||
|
DTXSID0022692
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
PRIMARY | |||
|
5XZM1R3DKF
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
PRIMARY | |||
|
m2729
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
PRIMARY | Merck Index | ||
|
260-964-5
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
PRIMARY | |||
|
BROTIZOLAM
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
PRIMARY | |||
|
19790
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
PRIMARY | RxNorm | ||
|
100000085858
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
PRIMARY | |||
|
2451
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
PRIMARY | |||
|
SUB05933MIG
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
PRIMARY | |||
|
C020960
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
PRIMARY | |||
|
57801-81-7
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
PRIMARY | |||
|
DB09017
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
PRIMARY | |||
|
409
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
PRIMARY | |||
|
CHEMBL32479
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
PRIMARY | |||
|
T-113
Created by
admin on Fri Dec 15 15:18:45 GMT 2023 , Edited by admin on Fri Dec 15 15:18:45 GMT 2023
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
IMPURITY -> PARENT |
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |