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
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
表单
solid
颜色
tan
溶解性
45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 0.8 mg/mL
H2O: insoluble
methanol: soluble
创始人
Roche
SMILES字符串
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
基因信息
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA5(2558), GABRA6(2559)
rat ... Gabrg1(140674)
应用
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.
生化/生理作用
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.
特点和优势
This compound was developed by Roche. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
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
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
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
Gian Marco Leggio et al.
Pharmacological research, 141, 384-391 (2019-01-17)
The dopamine D3 receptor (D3R), in the nucleus accumbens (NAc), plays an important role in alcohol reward mechanisms. The major neuronal type within the NAc is the GABAergic medium spiny neuron (MSN), whose activity is regulated by dopaminergic inputs. We
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