B6434
Bretazenil
≥96% (HPLC), solid
Synonym(s):
9H-Imidazo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepine-1-carboxylic acid, Ro 16-6028
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About This Item
Empirical Formula (Hill Notation):
C19H20N3O3Br
CAS Number:
Molecular Weight:
418.28
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Quality Level
assay
≥96% (HPLC)
form
solid
color
white
solubility
DMSO: 24 mg/mL, H2O: insoluble
originator
Roche
storage temp.
2-8°C
SMILES string
[H][C@@]12CCCN1C(=O)c3c(Br)cccc3-n4cnc(C(=O)OC(C)(C)C)c24
InChI
1S/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
InChI key
LWUDDYHYYNNIQI-ZDUSSCGKSA-N
General description
Bretazenil, a tetracyclic imidazocarboxylic ester, is an anxi-olytic/anticonvulsant agent. It possesses a half-life of 2.5 hours and is quickly absorbed.
Application
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.
Biochem/physiol Actions
Bretazenil is a benzodiazepine partial agonist.
Bretazenil is capable of binding to γ-aminobutyric acid type A (GABAA) receptors that are sensitive and insensitive to diazepam. This compound possesses negligible sedative or muscle relaxant effects.
Features and Benefits
This compound is a featured product for Neuroscience research. Click here to discover more featured Neuroscience products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound was developed by Roche. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
Regulatory Information
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Articles
DISCOVER Bioactive Small Molecules for Neuroscience
Anthony S Basile et al.
European journal of pharmacology, 500(1-3), 441-451 (2004-10-07)
Benzodiazepines remain widely used for the treatment of anxiety disorders despite a side-effect profile that includes sedation, myorelaxation, amnesia, and ataxia, and the potential for abuse. gamma-Aminobutyric acid(A) (GABA(A)) receptor partial agonists, subtype-selective agents, and compounds combining both of these
B O Ward et al.
Physiology & behavior, 68(4), 463-468 (2000-03-14)
Intraaccumbens infusions of the GABA(B) agonist baclofen are known to stimulate food intake in the rat. The aim of the present study was to evaluate the effects of baclofen infusion on nonfood-related chewing and on the consumption of a palatable
Joanna L Stanley et al.
Journal of psychopharmacology (Oxford, England), 19(3), 221-227 (2005-05-13)
The mouse rotarod test of motor coordination/sedation is commonly used to predict clinical sedation caused by novel drugs. However, past experience suggests that it lacks the desired degree of sensitivity to be predictive of effects in humans. For example, the
Global Trade Item Number
| SKU | GTIN |
|---|---|
| B6434-5MG | 04061832555508 |
| B6434-25MG | 04061832555492 |