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:
产品名称
Ro 15-4513, solid
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
SMILES string
CCOC(=O)c1ncn-2c1CN(C)C(=O)c3cc(ccc-23)N=[N+]=[N-]
InChI key
CFSOJZTUTOQNIA-UHFFFAOYSA-N
form
solid
color
tan
solubility
45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 0.8 mg/mL
H2O: insoluble
methanol: soluble
originator
Roche
Quality Level
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
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
Elli Leppä et al.
European journal of pharmacology, 666(1-3), 111-121 (2011-05-28)
The potent sedative-hypnotic zolpidem and the convulsant methyl-6,7-dimethoxy-4-ethyl-β-carboline-3-carboxylate (DMCM) act primarily by binding to the benzodiazepine site of the main inhibitory neurotransmitter receptor, the pentameric γ-aminobutyric acid type A receptor (GABA(A)). This binding depends critically on the wild-type F77 residue
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
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
Alexander Kuzmin et al.
Addiction biology, 17(1), 132-140 (2011-10-27)
The effects of repeated, intermittent administration of a moderate dose of ethanol (3.4 g/kg/day × 6 days, intragastrically via gavages) on cognitive function were examined in male Wistar rats. No significant differences in weight gain between the ethanol- and water-treated
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