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形狀
solid
顏色
tan
溶解度
45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 0.8 mg/mL
H2O: insoluble
methanol: soluble
起源
Roche
SMILES 字串
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 密鑰
CFSOJZTUTOQNIA-UHFFFAOYSA-N
基因資訊
human ... GABRA1(2554) , GABRA2(2555) , GABRA3(2556) , GABRA5(2558) , GABRA6(2559)
rat ... Gabrg1(140674)
應用
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.
特點和優勢
This compound was developed by Roche. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
個人防護裝備
Eyeshields, Gloves, type N95 (US)
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
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
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
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