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Merck

B6434

Bretazenil

≥96% (HPLC), solid

Synonim(y):

9H-Imidazo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepine-1-carboxylic acid, Ro 16-6028

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5 MG

920,00 zł

25 MG

3470,00 zł

920,00 zł


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Informacje o tej pozycji

Wzór empiryczny (zapis Hilla):
C19H20N3O3Br
Numer CAS:
Masa cząsteczkowa:
418.28
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:

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Nazwa produktu

Bretazenil, ≥96% (HPLC), solid

InChI key

LWUDDYHYYNNIQI-ZDUSSCGKSA-N

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

assay

≥96% (HPLC)

form

solid

color

white

solubility

DMSO: 24 mg/mL
H2O: insoluble

originator

Roche

storage temp.

2-8°C

Quality Level

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Ta pozycja
L9787SML0645SML1438
assay

≥96% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

form

solid

form

powder

form

powder

form

powder

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

2-8°C

storage temp.

-

storage temp.

2-8°C

storage temp.

−20°C

solubility

DMSO: 24 mg/mL, H2O: insoluble

solubility

DMSO: ≥6.0 mg/mL (Warmed), H2O: insoluble

solubility

DMSO: 5 mg/mL, clear (warmed)

solubility

DMSO: 10 mg/mL, clear

color

white

color

-

color

white to beige

color

yellow to orange

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).[1] 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.[2]

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.[3] This compound possesses negligible sedative or muscle relaxant effects.[4]

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.

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.[4]
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Klasa składowania

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)


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Dokumenty związane z niedawno zakupionymi produktami zostały zamieszczone w Bibliotece dokumentów.

Odwiedź Bibliotekę dokumentów

Aurélie Joly-Amado et al.
The EMBO journal, 31(22), 4276-4288 (2012-09-20)
Obesity-related diseases such as diabetes and dyslipidemia result from metabolic alterations including the defective conversion, storage and utilization of nutrients, but the central mechanisms that regulate this process of nutrient partitioning remain elusive. As positive regulators of feeding behaviour, agouti-related
L Mathiasen et al.
Psychopharmacology, 182(4), 475-484 (2005-09-01)
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. Conditioned models of anxiety were not assessed and are rarely encountered in phenotyping
Elisabetta Cagetti et al.
Molecular pharmacology, 63(1), 53-64 (2002-12-19)
One of the pharmacological targets of ethanol is the GABAA receptor (GABAR), whose function and expression are altered after chronic administration of ethanol. The details of the changes differ between experimental models. In the chronic intermittent ethanol (CIE) model for
A L van Steveninck et al.
British journal of clinical pharmacology, 41(6), 565-573 (1996-06-01)
1. Interaction between alcohol and bretazenil (a benzodiazepine partial agonist in animals) was studied with diazepam as a comparator in a randomized, double-blind, placebo controlled six-way cross over experiment in 12 healthy volunteers, aged 19-26 years. 2. Bretazenil (0.5 mg)
M Nazar et al.
Journal of neural transmission (Vienna, Austria : 1996), 106(5-6), 369-381 (1999-08-12)
The effects of an intrahippocampal administering of a nonselective full (midazolam), a partial benzodiazepine (BDZ) receptor agonist (bretazenil), and a BDZ1 selective (zolpidem) receptor ligand were examined in the open field test (OFT) of neophobia and Vogel's test (VT) of

Produkty

DISCOVER Bioactive Small Molecules for Neuroscience

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