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 is an alcohol antagonist.
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.
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.
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.
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
