Antioxidant BHT 264
CAS:128-37-0
Purity:99%
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Anti-anxiety agent.Bretazenil potentiated GABA responses on α4β3γ2 cells.Bretazenil is a partial benzodiazepine receptor agonist. Benzodiazepines, mainly diazepam, are commonly used as anticonvulsants in the treatment of organophosphate casualties. Bretazenil has been used to determine non-specific binding due to its affinity to bind to a variety of γ-aminobutyric acid type A (GABAA) receptor subtypes (α1-3;5). It has also been used as a GABAA receptor partial agonist in the subcutaneous Alzet minipumps to treat obese agouti related protein (AgRP) ablated and lean naive mice to study its effect on them.
(11aS)-6-bromo-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepine-5,11(10H)-dione
bretazenil
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps
1: NaH / dimethylformamide
2: tBuOK / dimethylformamide
With
potassium tert-butylate; sodium hydride;
In
N,N-dimethyl-formamide;
1: Substitution / 2: cyclocondensation;
|
tert-Butyl isocyanoacetate
phosphoric acid 6-bromo-5-oxo-2,3,5,11a-tetrahydro-1H-benzo[e]pyrrolo[1,2-a][1,4]diazepin-11-yl ester diethyl ester
bretazenil
Conditions | Yield |
---|---|
With
potassium tert-butylate;
In
N,N-dimethyl-formamide;
|
The CAS number of Bretazenil is 84379-13-5.
More information of Bretazenil 84379-13-5 are:
CAS Number |
84379-13-5 |
Density |
1.56 g/cm3 |
Boiling Point |
594.3 °C at 760 mmHg |
Flash Point |
313.2 °C |
Vapor Pressure |
4.29E-14mmHg at 25°C |
Refractive Index |
1.685 |
PSA |
64.43000 |
LogP |
3.81870 |
Pka |
0.78±0.20(Predicted) |
Synonyms for Bretazenil 84379-13-5:9H-Imidazo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepine-1-carboxylicacid, 8-bromo-11,12,13,13a-tetrahydro-9-oxo-, 1,1-dimethylethyl ester, (S)-;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 16-6028/000;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;8-Bromo-7-oxo-3b,4,5,6-tetrahydro-7H-2,6a,11b-triaza-benzo[g]cyclopenta[e]azulene-3-carboxylic acid tert-butyl ester;
The chemical formula of Bretazenil is C19H20BrN3O3 which containing 19 Carbon atoms,20 Hydrogen atoms,1 Bromine atoms,3 Nitrogen atoms and 3 Oxygen atoms,and the molecular weight of Bretazenil is 418.29.
Bretazenil is an imidazobenzodiazepine partial agonist and a potent anxiolytic. It is rapidly absorbed and has a half-life of 2.5 hours. Animal work has shown that, even after long-term administration of bretazenil, there are no changes in GABA receptor binding or function, and tolerance does not occur. Studies in humans have also suggested that bretazenil has a low abuse potential (Sellers et al. 1991). In terms of clinical effects, bretazenil has demonstrated anxiolytic efficacy in both generalized anxiety disorder and panic disorder (Katschnig et al. 1991), but no controlled study has compared bretazenil with a classic full agonist.
InChI:InChI=1/C19H20BrN3O3/c1-19(2,3)26-18(25)15-16-13-8-5-9-22(13)17(24)14-11(20)6-4-7-12(14)23(16)10-21-15/h4,6-7,10,13H,5,8-9H2,1-3H3/t13-/m0/s1
Relevant articles related to Bretazenil:
Article |
Source |
Synthesis of iodine-123 labelled analogues of the partial agonist (S)- and (R)-bretazenil for the study of CNS benzodiazepine receptors using SPECT |
Katsifis, Andrew,Mattner, Filomena,McPhee, Meredith,Kassiou, Michael,Najdovski, Ljubco,Dikic, Branko , p. 835 - 845 (2007/10/03) |
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