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:
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
Gene Information
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA5(2558), GABRA6(2559)
rat ... Gabrg1(140674)
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
此项目有
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
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
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| R109-100MG | 04061832273761 |
| R109-25MG | 04061832559513 |