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B6434

Bretazenil

≥96% (HPLC), solid

Sinónimos:

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

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Tamaño de envaseSKUDisponibilidadPrecio
25 mg
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653,00 €

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Fórmula empírica (notación de Hill):
C19H20N3O3Br
Número CAS:
Peso molecular:
418.28
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Assay:
≥96% (HPLC)
Form:
solid
Quality level:

653,00 €


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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.[1]

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).[2] 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.[3]

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.[4] This compound possesses negligible sedative or muscle relaxant effects.[1]

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.

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Este artículo
L9787SML0645SML1438
form

solid

form

powder

form

powder

form

powder

assay

≥96% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

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


Clase de almacenamiento

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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Artículos

DISCOVER Bioactive Small Molecules for Neuroscience


Bert Tuk et al.
Journal of pharmacokinetics and pharmacodynamics, 29(3), 235-250 (2002-11-27)
The pharmacokinetic and pharmacodynamic interactions of ethanol with the full benzodiazepine agonist midazolam, the partial agonist bretazenil and the benzodiazepine BZ1 receptor subtype selective agonist zolpidem have been determined in the rat in vivo, using an integrated pharmacokinetic-pharmacodynamic approach. Ethanol
D S Reddy et al.
Epilepsia, 42(3), 337-344 (2001-07-10)
Perimenstrual catamenial epilepsy may in part be due to withdrawal of the endogenous progesterone-derived neurosteroid allopregnanolone that potentiates gamma-aminobutyric acidA (GABA(A)) receptor-mediated inhibition. Here we sought to determine whether the anticonvulsant potencies of neuroactive steroids, benzodiazepines, phenobarbital (PB), and valproate
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



Número de artículo de comercio global

SKUGTIN
B6434-5MG04061832555508
B6434-25MG04061832555492

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