R109
Ro 15-4513
solid
Synonym(s):
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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About This Item
Empirical Formula (Hill Notation):
C15H14N6O3
CAS Number:
Molecular Weight:
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.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
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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
William T Ralvenius et al.
Nature communications, 6, 6803-6803 (2015-04-14)
Agonists at the benzodiazepine-binding site of GABAA receptors (BDZs) enhance synaptic inhibition through four subtypes (α1, α2, α3 and α5) of GABAA receptors (GABAAR). When applied to the spinal cord, they alleviate pathological pain; however, insufficient efficacy after systemic administration