溴他西尼

溴他西尼用途

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.

溴他西尼名称

[ CAS 号 ]:
84379-13-5

[ 中文名 ]:
溴他西尼

[ 英文名 ]:
Bretazenil

[英文别名 ]:

Ro 16-6028
Ro-16-6028
Bretazenil

溴他西尼物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 沸点 ]:
594.3±50.0 °C at 760 mmHg

[ 分子式 ]:
C₁₉H₂₀BrN₃O₃

[ 分子量 ]:
418.284

[ 闪点 ]:
313.2±30.1 °C

[ 精确质量 ]:
417.068787

[ PSA ]:
64.43000

[ LogP ]:
2.52

[ 外观性状 ]:
solid | white

[ 蒸汽压 ]:
0.0±1.7 mmHg at 25°C

[ 折射率 ]:
1.685

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
DMSO: 24 mg/mL, soluble

溴他西尼MSDS

详细MSDS(安全技术说明书)

溴他西尼毒性和生态

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

溴他西尼安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
22-24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
NJ5899850

溴他西尼合成路线

详细合成路线

溴他西尼上下游产品

溴他西尼上游产品

溴他西尼下游产品

溴他西尼文献

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...

更多文献