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Merck
CN

R109

Ro 15-4513

solid

别名:

Ethyl 8-azido-6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate, Ro15-4513

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关于此项目

经验公式(希尔记法):
C15H14N6O3
化学文摘社编号:
分子量:
326.31
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Form:
solid
Quality level:
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form

solid

Quality Level

color

tan

solubility

45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 0.8 mg/mL, H2O: insoluble, methanol: soluble

originator

Roche

SMILES string

CCOC(=O)c1ncn-2c1CN(C)C(=O)c3cc(ccc-23)N=[N+]=[N-]

InChI

1S/C15H14N6O3/c1-3-24-15(23)13-12-7-20(2)14(22)10-6-9(18-19-16)4-5-11(10)21(12)8-17-13/h4-6,8H,3,7H2,1-2H3

InChI key

CFSOJZTUTOQNIA-UHFFFAOYSA-N

Application

Ro 15-4513 has been used as a benzodiazepine (Bz) inverse agonist in rats and to test its binding with diazepam-sensitive (DS) receptors in in vitro radioligand binding studies.

Biochem/physiol Actions

Ro 15-4513 is benzodiazepine receptor partial inverse agonist. It elicits anxiogenic property and is an ethanol antagonist. It elicits a high affinity towards diazepam sensitive and insensitive sites in the cerebellar region. Ro 15-4513 possesses an imidazo ring and is an imidazobenzodiazepine.

Features and Benefits

This compound was developed by Roche. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

法规信息

新产品

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Franco R Mir et al.
British journal of pharmacology, 177(13), 3075-3090 (2020-03-07)
GABAA receptor functions are dependent on subunit composition, and, through their activation, GABA can exert trophic actions in immature neurons. Although several sex differences in GABA-mediated responses are known to be dependent on gonadal hormones, few studies have dealt with
P D Suzdak et al.
Science (New York, N.Y.), 234(4781), 1243-1247 (1986-12-05)
Ethanol, at pharmacologically relevant concentrations of 20 to 100 mM, stimulates gamma-aminobutyric (GABA) receptor-mediated uptake of 36Cl-labeled chlorine into isolated brain vesicles. One drug that acts at GABA-benzodiazepine receptors, the imidazobenzodiazepine Ro15-4513, has been found to be a potent antagonist
Anni-Maija Linden et al.
Frontiers in neuroscience, 5, 3-3 (2011-01-29)
Ethyl alcohol (ethanol) has many molecular targets in the nervous system, its potency at these sites being low compared to those of sedative drugs. This has made it difficult to discover ethanol's binding site(s). There are two putative binding sites
A M Kucken et al.
Molecular pharmacology, 57(5), 932-939 (2000-04-25)
gamma-Aminobutyric acid(A) receptor gamma-subunits are important for benzodiazepine (BZD) binding and modulation of the gamma-aminobutyric acid-mediated Cl(-) current. Previously, by using gamma2/alpha1 chimeric subunits, we identified two domains of the gamma2-subunit, Lys-41-Trp-82 and Arg-114-Asp-161, that are, in conjunction, necessary and
C Belzung et al.
Pharmacology, biochemistry, and behavior, 30(4), 867-870 (1988-08-01)
In order to better understand the antagonistic effects of the partial inverse agonist of benzodiazepine receptors, RO 15-4513, against the disinhibitory action of ethanol, we examined the effects of RO 15-4513 at a dose (2.0 mg/kg) that did not alter

全球贸易项目编号

货号GTIN
R109-100MG04061832273761
R109-25MG04061832559513

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