Bretazenil

Modify Date: 2024-01-06 19:06:59

Bretazenil Structure
Bretazenil structure
Common Name Bretazenil
CAS Number 84379-13-5 Molecular Weight 418.284
Density 1.6±0.1 g/cm3 Boiling Point 594.3±50.0 °C at 760 mmHg
Molecular Formula C19H20BrN3O3 Melting Point N/A
MSDS Chinese USA Flash Point 313.2±30.1 °C

 Use of Bretazenil


Bretazenil, also known as Ro 16-6028, is GABA A receptor agonist potentially for the treatment of anxiety disorders. Bretazenil differs from traditional 1,4-benzodiazepines by being a partial agonist and because it binds to α1, α2, α3, α4, α5 and α6 subunit containing GABAA receptor benzodiazepine receptor complexes. 1,4-benzodiazepines bind only to α1, α2, α3 and α5 GABAA benzodiazepine receptor complexes.

 Names

Name Bretazenil
Synonym More Synonyms

 Chemical & Physical Properties

Density 1.6±0.1 g/cm3
Boiling Point 594.3±50.0 °C at 760 mmHg
Molecular Formula C19H20BrN3O3
Molecular Weight 418.284
Flash Point 313.2±30.1 °C
Exact Mass 417.068787
PSA 64.43000
LogP 2.52
Appearance of Characters solid | white
Vapour Pressure 0.0±1.7 mmHg at 25°C
Index of Refraction 1.685
Storage condition 2-8°C
Water Solubility DMSO: 24 mg/mL, soluble

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
NJ5899850
CHEMICAL NAME :
9H-Imidazo(1,5-a)pyrrolo(2,1-c)(1,4)benzodiazepine-1- carboxylic acid, 11,12,13,13a- tetrahydro-8-bromo-9-oxo-, 1,1-dimethylethyl ester, (S)-
CAS REGISTRY NUMBER :
84379-13-5
LAST UPDATED :
199806
DATA ITEMS CITED :
1
MOLECULAR FORMULA :
C19-H20-Br-N3-O3
MOLECULAR WEIGHT :
418.33

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>312 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 13,730,1988

 Safety Information

Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Safety Phrases 22-24/25
RIDADR NONH for all modes of transport
WGK Germany 3
RTECS NJ5899850

 Precursor & DownStream

Precursor  1

DownStream  0

 Articles28

More Articles
A Comparison of the α2/3/5 Selective Positive Allosteric Modulators L-838,417 and TPA023 in Preclinical Models of Inflammatory and Neuropathic Pain.

Adv. Pharmacol. Sci. 2011 , 608912, (2011)

GABA(A) receptors containing α2/3 subunits are current targets in the battle to develop new pain medications, as they are expressed in the spinal cord where increasing inhibitory drive should result i...

A comparison of chlordiazepoxide, bretazenil, L838,417 and zolpidem in a validated mouse Vogel conflict test.

Psychopharmacology 182(4) , 475-84, (2005)

GABAA receptors containing an alpha2 subunit are proposed to mediate the anxiolytic effect of benzodiazepines (BZ) based on studies in transgenic mice using unconditioned models of anxiety. Conditione...

Contextual fear conditioning and baseline startle responses in the rat fear-potentiated startle test: a comparison of benzodiazepine/gamma-aminobutyric acid-A receptor agonists.

Behav. Pharmacol. 11(6) , 495-504, (2000)

In the rat, fear-potentiated startle (FPS) test animals are first trained to associate brief light presentations with a mild electric footshock and then tested for startle responses to acoustic stimul...

 Synonyms

tert-Butyl (13aS)-8-bromo-9-oxo-11,12,13,13a-tetrahydro-9H-imidazo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepine-1-carboxylate
2-Methyl-2-propanyl (13aS)-8-bromo-9-oxo-11,12,13,13a-tetrahydro-9H-imidazo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepine-1-carboxylate
9H-Imidazo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepine-1-carboxylic acid, 8-bromo-11,12,13,13a-tetrahydro-9-oxo-, 1,1-dimethylethyl ester, (13aS)-
Ro 16-6028
Ro-16-6028
tert-Butyl (S)-8-Bromo-11,12,13,13a-tetrahydro-9-oxo-9H-imidazo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepine-1-carboxylate
Bretazenil