RO 15-4513 Chemical Properties

storage temp. 

Desiccate at +4°C

solubility 

45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 0.8 mg/mL

form 

solid

color 

tan

CAS DataBase Reference

91917-65-6

Safety Information

WGK Germany 

3

MSDS

• Language:English Provider:SigmaAldrich

RO 15-4513 Usage And Synthesis

Description

Ro 15-4513 is a partial inverse agonist of benzodiazepine receptors. It acts as a competitive antagonist, and can therefore be an antidote to the acute impairment caused by alcohol. Ro 15-4513's Ki values are 3.1 and 5.3 nM for diazepam-insensitive (DI) and diazepam-sensitive (DS) benzodiazepine receptors respectively. Ro 15-4513 displays partial agonism at DI α4- and α6-GABAA receptors.

Chemical Properties

Off-white solid

Uses

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.

Uses

Ro 15-4513 is an alcohol antagonist.

Definition

ChEBI: 8-azido-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid ethyl ester is an organonitrogen heterocyclic compound and an organic heterotricyclic compound.

Application

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.

Biological Activity

High affinity benzodiazepine ligand. K i values are 3.1 and 5.3 nM for diazepam-insensitive (DI) and diazepam-sensitive (DS) benzodiazepine receptors respectively. Acts as partial inverse agonist at recombinant DS α 1-, α 2-, α 3- and α 5-GABA A receptors. Displays partial agonism at DI α 4- and α 6-GABA A receptors. Antagonizes several behavioral and neurochemical effects of ethanol. Proconvulsant and anxiogenic.

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.

storage

Desiccate at +4°C

RO 15-4513(91917-65-6)Related Product Information

• 4-Imidazolemethanol hydrochloride
• Methyl 4-imidazolecarboxylate
• Ethyl imidazole-4-carboxylate
• (1-METHYL-1H-IMIDAZOL-4-YL)METHANOL
• 5-Methyl-1H-imidazole-4-carbaldehyde
• 1H-Imidazole-4-carboxylic acid
• 4-(4-Methyl-1H-imidazol-1-yl)benzenamine
• 3-AMINO-N,N-DIMETHYLBENZYLAMINE
• 4-(1H-Imidazol-1-yl)aniline
• 4,5-DIMETHYL-1H-IMIDAZOLE
• ETHYL 5-METHYL-1H-IMIDAZOLE-4-CARBOXYLATE
• 1-METHYL-1H-IMIDAZOLE-4-CARBOXYLIC ACID METHYL ESTER
• Imidazole-4-methanol
• 1-Methyl-1H-imidazole-4-carboxylic acid
• 1-(1H-IMIDAZOL-2-YL)-ETHANOL
• 1,5-DIMETHYL-1H-IMIDAZOLE-4-CARBALDEHYDE
• 3-AMINO-N-ETHYLBENZAMIDE
• 3-AMINO-N,N-DIMETHYLBENZAMIDE